Scientific Program

Conference Series Ltd invites all the participants across the globe to attend 6th International Conference on Organic and Inorganic Chemistry Amsterdam, Netherlands.

Day 1 :

Conference Series Organic Chemistry 2019 International Conference Keynote Speaker Atef AbdelMoniem Kalmouch photo
Biography:

Atef AbdelMoniem Kalmouch has completed his PhD in the Faculty of Science at Zagazig University, Egypt. He is the Head of Peptide Chemistry Department, National Research Centre- Egypt. He has published more than 20 papers in reputed journals and has been serving as an Editorial Board Member of repute journals.

Abstract:

Dehydropeptides are significant constituents of several biologically active peptides. Accordingly, the class compounds present are useful synthetic precursors for assembling biologically active identities, namely, cytotoxic agents. Relative to the main peptide chain, the existence of the SP2 hybridized α-β atoms in the peptide chains limits the conformations of the side chains to either Z or E orientation at the Cβ carbon atom. This decreases the conformational flexibility, which makes the α-β dehyrodropeptide position and the amide backbone structurally suitable for building up some heterocyclic rings. The heterocyclic rings are, consequently, embedded in the peptide chain backbone as additional dehyro-peptidomimetics. Considerable research works towards their synthesis; structural, as well as, biological investigations are consequently, recently, explored. Herein, we will focus upon the synthesis and characterization of some tetrazols and oxadiazoles dehydro-peptidomimetics and their biological evaluation as cytotoxic, namely, anticancer agents against MCF-7 human breast carcinoma cells. The realized preliminary tests revealed that our nine tested compounds demonstrated cytotoxicity which was somewhat dose dependent. Five of them demonstrated high anticancer activity.

  • Aspects of Organic Chemistry | Medicinal and Bioorganic Chemistry | Green and Environmental Chemistry | Natural Products and Heterocyclic Chemistry | Analytical Chemistry
Speaker

Chair

Weiguo Cao

Shanghai University, China

Speaker
Biography:

Wei Zhou is currently enrolled in the Chemistry Department of Shanghai University as a MS student majoring in Organic Chemistry under the guidance of Professor Weiguo Cao. The group is committed to the synthesis of a series of perfluoroalkylated compounds. She published an article in the RSC Adv. and another in J. Org. Chem.

Abstract:

Pyrrolo[2,1-a]isoquinoline derivatives is a kind of compound with good fluorescence properties and also a kind of very important alkaloids having good biological activities. Therefore, the synthetic methodologies for constructing these compounds are highly demanded. DIPEA-promoted one-pot two-step threecomponent reaction for the synthesis of pyrrolo[2,1 a]isoquinoline has been achieved. In this paper, a series of perfluoroalkylated pyrrolo[2,1-a]isoquinoline derivatives (4) were synthesized by the reaction of isoquinolines (1), bromomethyl ketones (2) and methyl perfluoroalk-2-ynoates (3) in the presence of DIPEA (Scheme 1). This procedure is compatible with a broad range of functional groups in both pyridines and bromomethyl ketones with moderate to good yields.

Speaker
Biography:

Rasha Samir El-Tawil has completed her PhD from Cairo University, Egypt. She is a Researcher in Inorganic Chemistry Department at National Research Centre. She has published more than 10 papers in high impact factor scientific journals and has participated in more than six local projects.

Abstract:

Increasing needs to industry and world population growth led to the accumulation of a wide variety of contaminants in the environment. The effluents of wastewater in some industries such as textiles, leather, paper and plastics contain various kinds of synthetic dyes. Natural molecular sieves as silicate minerals contain tiny pores of precise and uniform size, which could be used as adsorbents, catalyst carriers and desiccants. In the present research, the Egyptian sand was used as adsorbent in the removal of methyl red dye from textiles effluents. The sand was processed by disposal of large sizes by dry sieving and disposal of small sizes by wet sieving. The sand was mechanically treated with grinding to reach the required porosity. The time factor and the effect of the grinding period were studied. X-ray diffraction (XRD), X-ray fluorescence (XRF) and size analysis were done for the sample before grinding. Complete physico-chemical characterizations of the textile effluent as pH, temperature, color, total dissolved solids (TDS), total suspended solids (TSS), chemical oxygen demand (COD), and biochemical oxygen demand (BOD) have been measured before and after treatment. The maximum color removal efficiency was found to be 91.45% of the methyl red dye from waste water.

Speaker
Biography:

Baljit Singh, (PhD) is a Professor of Chemistry in Himachal Pradesh University- Shimla-HP-India. He has about 19 years research and teaching experience. He has published more than 100 research papers in reputed journals and has guided seven PhD/20 MPhil students in the field of Polymer, Hydrogels and Drug Delivery Devices. He has handled many research projects. Presently, he is Professor and Chairman in the Department of Chemistry at Himachal Pradesh University Shimla.

Abstract:

Keeping in view the inherent wound healing ability of polysaccharides, tragacanth gum and sodium alginate, in the present work, an attempt has been made by my research group to design the antibiotic drug ‘gentamicin’ and analgesic drug ‘lidocaine’ loaded sterile hydrogel dressings by radiation induced crosslinking, for simultaneous care of wound infection and wound pain. These polymers were characterized by cryo-SEM, AFM, FTIR, XRD, 13C-NMR, and swelling studies. Drug release profile and other biomedical properties like haemolysis, mucoadhesion, water vapor permeability, microbial penetration, antioxidant activities and oxygen permeability were also determined. The results showed that wound fluid absorption and slow drug release ability of hydrogel films. These polymer films were found to be blood compatible, permeable to water vapor and O2, and impermeable to microorganism. Further, the synergic effects of antimicrobial and antioxidant nature of hydrogel dressings will make them suitable candidate for wound management.

Speaker
Biography:

Shubhashish has obtained his BS-MS dual degree in Chemistry from Indian Institute of Science Education and Research, Bhopal. Then in 2016, he moved to USA, University of Connecticut for Doctoral studies in the Department of Chemistry under the supervision of Prof. Steven Suib. His work mostly focuses on catalysis and its application in organic transformation.

Abstract:

Oxidative coupling of amine to imine is very well-known process and has been extensively studied before. However, work on highly selective oxidative coupling is limited. In this work we have synthesized a molybdenum oxide mesoporous heterogeneous catalytic system. Through Brunauer–Emmett–Teller (BET) we confirmed that this material is mesoporous in nature. To check the crystallinity, X-ray diffraction was done and an orthorhombic cubic system was determined, which is different from commercially available molybdenum oxide which is monoclinic. Diffuse reflectance ultraviolet−visible spectra show that there is a blue shift in the spectra compared to commercially available molybdenum oxide. Scanning electron microscopy (SEM) and Tunneling electron microscopy (TEM) were done to study the morphology. This catalytic system was then used for amine coupling to form imines. Under very simple reaction conditions selectivities, conversions, and turn over numbers were observed to be very high.

Speaker
Biography:

Xiaoli Sun is 24 years old and currently enrolled in the Chemistry Department of Shanghai University as a MS student majoring in organic chemistry under the guidance of Professor Weiguo Cao. The group is committed to the synthesis of a series of perfluoroalkylated compounds.

Abstract:

Fluorene derivatives have attracted wide spread interest because of their important applications in the fields of biomedical and photoelectric materials. Moreover, they are also effective ligands in organometallic chemistry and unique protecting groups in peptide synthesis. In recent years, the photoelectrical potential of fluorene and related derivatives has become well recognized. Herein we report a novel and efficient metal-free method for the synthesis of perfluoroalkylated fluorenylphosphonate derivatives 4 involving the reaction of 1-indanones 1, malononitrile 2 and perfluoroalkynyl phosphonates 3 (Scheme 1). A series of perfluoroalkylated fluorenylphosphonate derivatives 4 were synthesized in moderate to good yields.

Speaker
Biography:

Senem Akkoç has obtained her Bachelor’s Degree from Bülent Ecevit (Zonguldak Karaelmas) University in 2009. She has completed her Master’s degree in the synthesis and properties of N-heterocyclic salts at Inonu University in 2012. She has completed her PhD from Erciyes University about in-vitro cytotoxic activity of synthesized benzimidazolium salts. She had been in the University of Sydney (Australia) as a Visiting Scholar from 2015 to 2016. She has
published more than 30 papers in reputed journals and has been serving as an Editorial Board Member of three journals.

Abstract:

Yann Trolez

Ecole Nationale Supérieure de Chimie de Rennes (Univ Rennes), France

Title: Reactivity of ynamides with tetracyanoethylene: Formation of new electron super-acceptor
Speaker
Biography:

Yann Trolez has completed his PhD in 2010 from the University of Strasbourg under the guidance of Jean-Paul Collin and Jean-Pierre Sauvage where he worked on rotaxanebased molecular machines. He then moved to ETH Zürich in François Diederich group as a Post-doctoral fellow where he worked on alleno-acetylenic compounds bearing interesting optoelectronic properties. In 2011, he was appointed as Assistant Professor at the Ecole Nationale Supérieure de Chimie de Rennes (Univ Rennes) where he now works on organic interstellar chemistry and on new cyanated compounds having interesting optical properties. He has published about 35 papers in peer-review international journals.

Abstract:

Tetracyanoethylene (TCNE) is well known for reacting with some electron-rich alkynes to lead to 1,1,4,4-tetracyanobutadiene (TCBD) moieties in variable yields. This reaction processes according to a [2+2] cycloaddition followed by a [2+2]retroelectrocyclization. Some of the corresponding products have interesting opto-electronic properties, in particular in non-linear optics. However, this reactivity had never been tested with ynamides, which are electron rich alkynes where a nitrogen is directly linked to the triple bond. We recently demonstrated that ynamides easily react with TCNE at room temperature to give TCBDs in generally high yields (Figure 1). This reaction is very tolerant to many substituents. These new TCBDs are electron super-acceptors: indeed, according to electrochemical studies, they can be reduced around -0.1 and -0.6 V vs. SCE (two distinct reversible reduction waves in cyclic voltametry). We showed that they could dramatically influence the absorption properties of the substrate they are linked to. We also explored the possibility to run the reaction with more complex ynamides. In the presentation, we will present the scope of the reaction with a series of various ynamides. Some original optical and electronic properties will also be discussed.

Speaker
Biography:

Hayam Abd El Rahman Abd El Salam has completed her PhD from the Faculty of Science Ain Shams University. She is a Researcher in Green Chemistry Department, National Research Center, Dokki, Giza, Egypt. She has published more than seven papers in reputed journals and experience in extraction of natural organic compounds from many fatty wastes such as (swap stock, oils, free fatty waste) and used some extracted compound as complexing agents after modified the structure of this compounds.

Abstract:

This research involved structural and molecular behaviour of the ligand HL, 4-amino-5-(2,2-dichloro-1-methylcyclopropyl)-4H-1,2,4-triazole- 3-thiol towards the transition metal ions namely Cu(II), Zn(II) and Cd(II) had been studied using magnetic, electronic, elemental analyses, 1H-NMR, FT-IR and thermal analyses (TGA and DTA). The interpretation of practical data obtained had been evaluated and confirmed by theoretical molecular modelling. The computations had been done by software of Gaussian 09 W package. The geometries of traizole-thiole ligand and its metal chelates were fully optimized using density functional theory B3LYP method. There are no symmetry constrains had been applied during geometry optimization. (DFT)/GENECP level by implementing Def2TZVP basis set was used for Cu, Cd and Zn-atoms; and basis set 6-311++G (d, p) was used for other atoms. The mixed basis set had been selected due to its flexibility. HOMO and LUMO energy values for chelates, chemical hardness and electronegativity had been calculated. NBO calculations had been done at the same level using (NBO 3.1) program involved in the software of Gaussian 09 W for measuring the intra-molecular delocalization in systems under investigation qualitatively. TD-DFT approximation at the same level of theory was used to calculate the electronic absorption spectra of the studied chelates. Their structures were confirmed via correlation between experimental and theoretical calculations. The antimicrobial results of the ligand and its metal chelates had been recorded against two bacteria positive (Escherichia coli) and negative (Staphylococcus aureus) and two fungus (Aspergillus flavus and Candida albicans).

Speaker
Biography:

Nazila Gholipour has completed her PhD in Radiopharmacy in 2013 from Tehran University of Medical Sciences. She is a Faculty Member at Baqiyatallah University of Medical Sciences as an Assistant Professor from 2014 until now.

Abstract:

In recent decades, new drug delivery systems that have vital applications in targeted and specialized therapies are on the rise. These researches have provided a good basis for the use of new carriers, including the porous metal-organic framework (MOF), in targeted drug delivery systems. In this research, the magnetic MIL-100 was prepared using the hydrothermal methods. Also, these nanostructures were coated with folate-chitosan. The obtained magnetic carriers characterized by various techniques such as X-ray diffraction, field emission-scanning electron microscopy, transmission electron microscopy, vibrating sample magnetometer and Fourier transform infrared. The effect of hydrothermal conditions e.g. temperature, solvent and metal to ligand ratio on the morphology and size of prepared nanocomposites have been investigated. The sizes of magnetic nanoparticles have an impact effect on the drug encapsulation efficiency and release performance. The in-vitro release of curcumin from MIL-100@Fe3O4/chitosan carriers was investigated. Curcumin was efficiently released from magnetic carriers into environment under acidic pHs.

  • Poster Presentation
Location: Foyer
Speaker
Biography:

Senem Akkoç has obtained her Bachelor’s Degree from Bülent Ecevit (Zonguldak Karaelmas) University in 2009. She has completed her Master’s degree in the synthesis and properties of N-heterocyclic salts at the Inonu University in 2012. She has completed her PhD from Erciyes University about in-vitro cytotoxic activity of synthesized benzimidazolium salts. She had been in the University of Sydney (Australia) as a Visiting Scholar from 2015 to 2016. She has published more than 30 papers in reputed journals.

 

Abstract:

For the formation of C-C bonds in the midst of the organoboron compounds and organic halides, Pd-catalyzed Suzuki-Miyaura cross-coupling reaction is a very important method. The aryl chlorides have usually been used as substrates for this reaction due to practical and economic reasons. A series of unsymmetrical substituted new benzimidazolium salts and their PEPPSI type palladium complexes, which have become popular in recent years, were synthesized in order to improving more reactive catalysts. For the synthesis of salts, firstly, 1-alkylbenzimidazole was prepared from benzimidazole (1 mmol), alkyl chloride (1 mmol) and potassium hydroxide (1 mmol) in ethyl alcohol (60 mL). Alkyl halide (1 mmol) was added to a solution of DMF containing 1-alkylbenzimidazole (1 mmol) and the reaction mixture was refluxed for 24 h. On the other hand, PEPPSI type Pd-NHC complexes were prepared from PdCl2 (1 mmol), benzimidazolium salts (1 mmol) and K2CO3 (5 mmol) in 3-chloropyridine (3 mL). The structures of all compounds were characterized by suitable spectroscopic and analytic methods. All compounds were tested as catalysts in Suzuki-Miyaura reaction, which was done using following reagents; organoborane derivatives, aryl halides, synthesized compounds, base and DMF/H2O. The reaction mixture was sustained at different temperatures and times for obtaining optimum conditions. According to the obtained results, they especially were quite effective in the coupling of 4-chlorotoluene with 4-tertbutylphenylboronic acid.

Speaker
Biography:

Weiguo Cao has obtained his PhD degree from Shanghai Institute of Applied Physics, Chinese Academy of Sciences in 2003. Currently, he is working in Department of Chemistry at Shanghai University. He has been focusing on the development of synthetic methodologies for the constructing of fluorinated heterocycles using fluorine-containing building blocks with more than 300 papers.

Abstract:

Fused pyrroles are ubiquitous motifs in a substantial number of naturally and non-naturally occurring compounds and can often serve as “privileged structures” in medical and pharmaceutical chemistry. Among them, pyrano[3,4-c]pyrrole derivatives have aroused interest owing to their biological activities. Herein, we report the efficient and stereoselective synthesis of trifluoromethylated pyrano[3,4-c]pyrroles via three-component bicyclization process. We performed the reaction by employing 3-aroylacrylic acids 1, methyl 4,4,4-trifluorobut-2-ynoate 2 and tert-butyl isocyanide 2 in MeCN. After stirring for 12 h at 80ï‚°C, a series of trifluoromethylated pyrano[3,4-c]pyrroles 4 were synthesized in good to excellent yields

Speaker
Biography:

An efficient highly convenient synthesis of polysubstituted pyridine derivatives was established via the reaction of N-(benzothiazol-2-yl)-2-cyanoacetamides with an assortment of arylidene malononitrile or arylidene ethyl cyanoacetate in the presence of L-Proline as efficient organocatalyst for such type of ultrasonic-mediated Michael addition. The mechanistic pathway and the factors affecting this reaction were also established. The main characteristics of this procedure are high yields, utilizing a cost-effective catalyst, ease of work-up and purification ways.

Abstract:

Haider Behbehani has completed his PhD from Bath University, UK and Post-doctoral studies from Bath University School of Organic Chemistry. He is the Assistant Vice President for Research Analysis and Development. He has published more than 40 papers in reputed journals and has been serving as an Editorial Board Member of repute.

Speaker
Biography:

Wafa A Baker Bawazir has gained her Philosophy Doctoral of Organic Chemistry in 2016, thesis entitled “Tandem Reactions to Synthesise sp3 Rich Skeletons”, school of Chemistry at The University of Nottingham, United Kingdom. In 2009, she gained her MSc Organic Chemistry, thesis entitled as “Synthesis of Some More Fluorine Compounds derived from Sulfa Drugs as Biological Agents”. She has worked as a Lecturer in Faculty of Medicine and Applied Science at KAU for seven years. Since May 2018, she became the Chairwoman of Chemistry Department, King AbdulAziz University. Her research interests are Synthesis of novel 1,2,4-triazine Derivatives Systems, Medicinal Chemistry Synthesis and SAR studies of compounds, Synthesis of Biologically Active Compounds, E-Learning in Chemistry, Sustainability in Chemistry and Pollutants.

Abstract:

During last decade, many classes of azathio crown macrocycles containing two 1,2,4-triazine rings as bioactive subunits have been approached for building of a new chemotherapy antitumor drugs. Sun et al. prepared a stable type of ruthenium complexes containing 3-amino-1,2,4-triazino[5,6-f]1,10-phenanthroline and reported their electrochemical and photophysical properties. Based on these facts, the purpose of this work is to extend and explore more on the scope of our previous studies fluorine substituted 1,2,4-triazines heterocyclic rings was used in order to enhance the complex as CDK2 inhibitors of tumor cell. Novel fluorinated class of cyclic aza-oxo crown macrocyclic systems containing 1,2,4-triazinone moieties (6) and their Ru-complexes 7 have been obtained from the interaction between 5,6-di(4-fluorophenyl)-3-mercapto-1,2,4-triazine (1) with 2,6-diaminopyridine (2) followed by ring closer reaction with diethyl oxalate and reflux with RuCl3.xH2O in N,N-dimethylaniline to afford the Ru-complex. Structures of the products were deduced from their elemental analysis and spectral measurements.

Speaker
Biography:

Senem Akkoç has obtained her Bachelor’s Degree from Bülent Ecevit (Zonguldak Karaelmas) University in 2009. She has completed her Master’s degree on the synthesis and properties of N-heterocyclic salts at Inonu University in 2012. She has completed her PhD from Erciyes University about in-vitro cytotoxic activity of synthesized benzimidazolium salts. She had been in the University of Sydney (Australia) as a Visiting Scholar from 2015 to 2016. She has published more than 30 papers in reputed journals.

Abstract:

In the past few decades, infections caused by multi-drug resistant bacteria have increased at frightening levels all over the world. Microbial infections are a growing health problem in modern medicine and the use of antibiotics is widespread in the worldwide. In particular, infections caused by the Gram-positive bacterium Staphylococcus aureus and species of the genus Enterococcus have become a major worldwide health problem due to their ability to develop resistance to multiple antibiotics. To overcome these emerging resistance problems, there is an urgent need to discover novel chemotherapeutic agents, which have a broad spectrum of activity and, if possible, with new modes of action. A series of benzimidazolium salts were synthesized and their structures were completely verified by means of elemental analysis, FT-IR, 1D NMR: 1H NMR, 13C NMR. The biological activities of these salts were examined and were found to show moderate activity. The synthesized n-butyl substituted salt displayed the best activity against A. hydrophila, P. aeruginosa, E. coli, S. aureus and L. monocytogenes as Gram +/- microorganisms. The synthesized ethyl substituted salt showed significant activity compared to the other salts against S. typhimurium and Y. enterocolitica. Finally, it could be concluded that nearly all compounds exerted moderate antibacterial activity.

Speaker
Biography:

Amanda Perumal has completed her Master of Science in Biochemistry in 2016. She is currently pursuing her Doctoral degree in Synthetic Organic Chemistry at the University of KwaZulu-Natal, South Africa. She thoroughly enjoys her research and has keen interest in drug development targeting life threatening diseases.

Abstract:

Quinoline is a nitrogen-containing heterocyclic aromatic structure with chemical formula C9H7N and is characterized by a benzene ring fused to a pyridine ring at two adjacent carbons. Quinoline and its derivatives have been the focus of considerable scientific and clinical interest due to their wide range of biological applications, such as antibacterial, antifungal, antimalarial, anticancer and immune depressing activities to name a few. The quinoline scaffold is prevalent in a variety of pharmacologically active synthetic and natural compounds. Twelve novel 2-Methyl quinolines were successfully synthesized by the Doebner-Miller reaction using crotonaldehyde and anilines. These quinolines were functionalised by oxidising the 2-methyl group with selenium dioxide and the resultant carbaldehyde used as an intermediate to a variety of syntheses. In this project, focus was on the synthesis of imines with various anilines, conversion of these imines to ß-lactams using phenoxy acetyl chloride. Characterization and structural elucidation of the novel synthesised molecules by NMR spectroscopy and mass spectrometry were performed. The synthesised quinoline derivatives were subjected to in-vitro screening for antimicrobial and anticancer activity. A structure-activity relationship was then carried out and the most active compounds were identified.

Speaker
Biography:

Ragab Abd Eltawab Abd El-Latief is a Researcher in Egyptian Petroleum Research Institute (EPRI), Petroleum Applications Department at Asphalt Lab. He has publications of books entitled “Environmentally Friendly and Economical Road Construction”, “Manufacture of Specific Asphalt Binder for Use in Paving by using Waste and Low Cost Materials”, LAP LAMBERT Academic Publishing (2014). He has a publication of a chapter in a book entitled "Using of Waste and Low Cost Materials in Manufacture of Specific Asphalt Binder for Use in Paving  Vol.2: Petrochemical of Adv. in Petroleum Engineering, Studium Press, LLC, USA. (2014). He is a Key Member of the project: Enhancing Sinai Population: Novel Modification of Soft Asphalt for Use in Roadway Network Development and Infrastructure Applications.

Abstract:

High construction costs when combined with awareness regarding environmental stewardship have encouraged the use of waste and renewable resources in asphalt modification. Increasing energy costs and the strong worldwide demand for petroleum has encouraged the development of alternative binders to modify or replace asphalt binders. The benefits of using alternative binders are that they can help save natural resources and reduce energy consumption while maintaining and, in some cases improving asphalt performance. Use of alternative (or byproduct) materials in asphalt mixtures may be one of the most complicated of the highway uses. The best use must be carefully engineered and designed, including the design of the mixture itself, the effects of the alternative materials on the asphalt binder behavior, and the pavement into which it will be incorporated. Common alternative has been observed that most, if not all, of these alternative binders contain chemical compositions somewhat similar to those of conventional asphalt binders (e.g. hydrocarbons, aromatics, saturates, and asphalt). However, tests indicate significant variability in the properties of alternative binders. In addition, the modification mechanism (chemical) for asphalt with alternative binders depends on the base asphalt and is therefore not well understood. It is critical to evaluate the technical feasibility of incorporating alternative binders into conventional asphalt binders for use in pavements. Because of the urgent need for infrastructure rehabilitation and maintenance, the introduction and application of such sustainable and environmentally friendly materials will have significant impact on the national economy as well as energy sustainability. It is necessary to determine what types of byproduct materials are suitable for use as alternative binders. Any alternative material under consideration must be adequate in chemical composition so that the asphalt material can be compatible using the highest amount of alternative binder possible. Considering the urgent need for infrastructure rehabilitation, the introduction and application of these sustainable and environmentally friendly materials could have significant impacts on the national economy as well as energy sustainability.

Speaker
Biography:

Senem Akkoç has obtained her Bachelor’s Degree from Bülent Ecevit (Zonguldak Karaelmas) University in 2009. She has completed her Master’s degree in the synthesis and properties of N-heterocyclic salts at Inonu University in 2012. She has completed her PhD from Erciyes University about in-vitro cytotoxic activity of synthesized benzimidazolium salts. She had been in the University of Sydney (Australia) as a Visiting Scholar from 2015 to 2016. She has published more than 30 papers in reputed journals and has been serving as an Editorial Board Member of three journals.

Abstract:

Benzimidazole and its derivatives demonstrate pharmacological activities and they also have a significant role as therapeutic agents. For example: there are few drugs containing benzimidazole nucleus showing following biological activity such as fungicidal, bactericidal, analgesic, anticancer and antiviral properties. The 5,6-dimethyl-1-(α-D-ribofuranosyl) benzimidazole ring system as an integral part of the structure of vitamin B12, which is discovered by Bonnett in 1948, is also including benzimidazole nucleus. Here, four new benzimidazolium salts were synthesized and characterized by 1H NMR, 13C NMR, IR and elemental analysis (Figure 1). Energy values of salts were calculated using the Spartan 10 program. The cytotoxic activities of compounds were determined as testing against the following cell lines: DLD-1, MDA-MB-231, HepG2, Beas-2B, HEK-293T using MTT assay methods for in-vitro cytotoxicity. Cisplatin was used as positive control drug. As a result, all organic compounds exhibited akin to or better results than cisplatin against the tested cell lines, and hence can be considered for further development for cancer therapy. Furthermore, microscopic examination of cells was done using Leica inverted microscopy and Olympus confocal microscope.

Aigul Ye. Malmakova

A.B. Bekturov Institute of Chemical Sciences, Kazakhstan

Title: IR and NMR studies of drugs complexation with β-Cyclodextrin
Speaker
Biography:

Aigul Ye Malmakova has completed her PhD from Kazakh-British Technical University. She is the Scientific Secretary and Senior Researcher in Laboratory of Chemistry of Synthetic and Natural Medicinal Compounds at A.B. Bekturov Institute of Chemical Sciences. She has published more than 20 papers, 51 abstracts of conferences and 12 patents of Republic of Kazakhstan and has been serving as an Executive Secretary of Chemical Journal of Kazakhstan.

Abstract:

β-cyclodextrin (β-CD) is widely used to increase stability and solubility of drugs in water, to increase the bioavailability of drugs, etc., to reduce the side effects of Dimedrol, Clophelin and Tolperisone. Their β-CD inclusion complexes were obtained with dissolving of drug (as hydrochloride and/or base) and β-CD via slow addition of drug solution to the β-CD solution. The formation of inclusion complexes were affirming by IR and NMR spectroscopy. Using the example of a comparative analysis of IR spectra (Сlophelin-base or Dimedrol-base, β-CD and its complexes, Fig. 1 and Fig. 2), it was shown that resulting crystalline product was a physical mixture of Сlophelin-base and β-CD (Fig. 1). While the spectrum of complex of Dimedrol-base+β-CD was characterized by absence of absorption bands observed in drug spectrum at 746.8; 700.8 and 2770-3030 cm-1, related to aromatics. This suggests the formation of inclusion complex by the “occurrence” of both phenyls of Dimedrol into the β-CD cavity, i.e. “guest”-“host”=1:2. Evidence of inclusion of Dimedrol-base molecule into the β-CD internal cavity by the 1Н NMR spectroscopy was a change in the chemical shifts of the protons H-3 (-0.18), H-5 (0.09) and H-6 (0.18), directed into the internal cavity β-CD molecules and exposed to the incorporated molecule. On the other hand, the descreening of H-9 (-0.22) and C-7 (-1.17), C-9 (-0.24) and C-10 (-0.54) and the screening of both Cq (1.41) Dimedrol's phenyl fragments showed that both phenyl were incorporated into an internal cavity of two β-CD.

Speaker
Biography:

Abstract:

The need for quantifying more inorganic elements susceptible of being present in the environment at very low concentrations due to the issues of traceability, authentication and safety urges the development of more efficient methodologies for sample preparation. Multielemental analysis of olive oil by ICP-MS is challenging due to the risk of matrix effects caused by the high organic load of the samples. Sample preparation aims at mitigating these issues, however, conflicting standard operating procedures in preparation of olive oils prior to ICP-MS analysis have been reported. This study compared two current practices of microwave-assisted acid digestion, and liquid-liquid ultrasound-assisted extraction methods with an optimized combined microwave digestion-evaporation method to extract inorganic elements from olive oils. The main objective of this study is to develop a robust preparation method which allows the accurate and precise quantification by ICP-MS of major and trace elements in olive oil samples. The method and programs for these three methods are described and their results are compared to aid choosing the method that reaches higher performance judged by lower detection limits, higher sensitivity and higher precision. Overall, microwave digestion-based methods did not compare opportunely, and ultrasound-assisted extraction was found to provide the best accord between simplicity of use, detection limits and precision improvement. The ultrasound-assisted extraction is therefore recommended as a preparation method for olive oils prior to analysis by ICP-MS. The broader range of elements that can be accurately detected is expected a help to increase the discriminatory power and performance of geographical traceability models.

Speaker
Biography:

Martin Kamlar completed his PhD in 2015 at Charles University, Czech Republic. After three years working as a postdoctoral fellow and Assistant Professor at the same university, he received a scientific internship and moved to Gothenburg in Sweden. He currently works in the research group of Professor Sundén at Chalmers University of Technology.

Abstract:

Carbon-carbon bond formation is a fundamental transformation in synthetic organic chemistry. Hence, many transformations leading to C-C bond formation have been developed and then used in synthesis of simple and complex molecules. In recent years considerable attention has been given to increase the efficiency of organic synthesis, particularly by reducing of chemical waste and production cost. One option to meet these criteria are domino reactions. This method involves the formation of several bonds under the same reaction conditions without adding additional reagents, catalysts, or isolating the reaction intermediates.1 With respect to our previous research,2 we turned our attention to OxoTriphenylHexanOates (1, OTHOs) due to their easy accessibility via a threecomponent ionic liquid promoted reaction. The treatment of corresponding OTHOs with boron tribromide lead to the formation of tetracyclic molecules 2, in good yields of up to 74%, via the reaction sequence involving the formation of three new C-C bonds.

Speaker
Biography:

Yang Ou studied medicinal chemistry at the Peking University, acquiring his Master's degree in 2015. He is currently working towards his PhD at Ruhr-Universität Bochum under the supervision of Prof. Lukas J. Goossen. His research program is focused on the development of new strategies to access fluorinated molecules and heterocycles.

Abstract:

Substituted styrenes are key building blocks in organic synthesis, and are widely used in the manufacturing of fine chemicals and polymers. Moreover, the vinyl group can be used as a hub for further functionalization, for example, by olefin metathesis, carboxylation, (asymmetric) hydrofunctionalization, or heterocycle synthesis. Acrylic acid is presented as an inexpensive, nonvolatile vinylating agent in a palladium-catalyzed decarboxylative vinylation of aryl halides. The reaction proceeds through a Heck reaction of acrylic acid, immediately followed by protodecarboxylation of the cinnamic acid intermediate. The use of the carboxylate group as a deciduous directing group ensures high selectivity for monoarylated products. The vinylation process is generally applicable to diversely substituted substrates. Its utility is shown by the synthesis of drug-like molecules and the gram-scale preparation of key intermediates in drug synthesis.