Day :
- A Trend in The Chemistry of Ketengem-Dithiol Reaction and Transformations .
Session Introduction
Salem E. Zayed
Lecturer at University of South Valley
Title: A Trend in The Chemistry of Ketengem-Dithiol Reaction and Transformations
Biography:
Salem E. Zayed Is a Lecturer at University of South Valley and his research field includes the Synthesis of some new sulfur content compounds ( in the form of thiols,
thiones, hetrocyclic sulfur and/or combined with other elements), and
study the biological activities. e. g. Anticancer, Tuberculoses, and anti-
infecte micro-organisms like Bacteria, Fungi.
Abstract:
Acid catalyzed reaction of 1-(1H-indol-3-yl)-3,3-dimercaptoprop-2-en-1-one (1) with anthranilic acid (2) was achieved to produce 2-(1H-indol-3-yl)-4-oxo-1,4-dihydroquinoline-3-carbodithioic acid (3). Reactions of (1) with some amines e.g. p-chloroaniline (4) and o-aminophenol (5) in equimolar ratios and different reaction conditions were explored to produce (E)-3-((4-chlorophenyl)imino)-3-(1H-indol-3-yl)prop-1-ene-1,1-dithiol (6) and (E)-2-(benzo[d]oxazol-2(3H)-ylidene)-1-(1H-indol-3-yl)ethan-1-one (7) respectively. While reaction of (1) with 3,5- dibromosalicyldehyde (8) or glucose (9), (6,8-dibromo-4-hydroxy-2-mercaptochroman-3-yl)(1H-indol-3-yl)methanone (10) and 2-(dimercaptomethylene)-3,4,5,6,7,8-hexahydroxy-1-(1H-indol-3-yl)octan-1-one (11) were obtained respectively. Also 5-(1H-indol-3-yl)-3H-1,2-dithiole-3-thione (12) was obtained from the reaction of (1) with P2S5. On treatment (12) with different reagents as 3,5-dibromosalicyldehyde (8) and anthranilic acid (2) gave the adducts 6,8-dibromo-3-(1H-indol-3-yl)-9a-mercapto-3H,9aH-[1,2]dithiolo[3,4-b]chromen-4-ol (13) and 3-(1H-indol-3-yl)-9a-mercapto-9,9a-dihydro-4H-[1,2]dithiolo[3,4-b]quinolin-4-one (14) respectively
Salem E. Zayed
Lecturer at University of South Valley
Title: A Trend in The Chemistry of Ketengem-Dithiol Reaction and Transformations
Biography:
Salem E. Zayed Is a Lecturer at University of South Valley and his research field includes the Synthesis of some new sulfur content compounds ( in the form of thiols,thiones, hetrocyclic sulfur and/or combined with other elements), andstudy the biological activities. e. g. Anticancer, Tuberculoses, and anti- infecte micro-organisms like Bacteria, Fungi.
Abstract:
Acid catalyzed reaction of 1-(1H-indol-3-yl)-3,3-dimercaptoprop-2-en-1-one (1) with anthranilic acid (2) was achieved to produce 2-(1H-indol-3-yl)-4-oxo-1,4-dihydroquinoline-3-carbodithioic acid (3). Reactions of (1) with some amines e.g. p-chloroaniline (4) and o-aminophenol (5) in equimolar ratios and different reaction conditions were explored to produce (E)-3-((4-chlorophenyl)imino)-3-(1H-indol-3-yl)prop-1-ene-1,1-dithiol (6) and (E)-2-(benzo[d]oxazol-2(3H)-ylidene)-1-(1H-indol-3-yl)ethan-1-one (7) respectively. While reaction of (1) with 3,5- dibromosalicyldehyde (8) or glucose (9), (6,8-dibromo-4-hydroxy-2-mercaptochroman-3-yl)(1H-indol-3-yl)methanone (10) and 2-(dimercaptomethylene)-3,4,5,6,7,8-hexahydroxy-1-(1H-indol-3-yl)octan-1-one (11) were obtained respectively. Also 5-(1H-indol-3-yl)-3H-1,2-dithiole-3-thione (12) was obtained from the reaction of (1) with P2S5. On treatment (12) with different reagents as 3,5-dibromosalicyldehyde (8) and anthranilic acid (2) gave the adducts 6,8-dibromo-3-(1H-indol-3-yl)-9a-mercapto-3H,9aH-[1,2]dithiolo[3,4-b]chromen-4-ol (13) and 3-(1H-indol-3-yl)-9a-mercapto-9,9a-dihydro-4H-[1,2]dithiolo[3,4-b]quinolin-4-one (14) respectively
Tao Wang
Master`s degree in “Medicinal Chemistry†from the University of Guizhou
Title: Novel Multivalent Glyco-gold Nanoparticles to Inhibit Bacterial Fim H
Biography:
Tao WANG received his Master`s degree in “Medicinal Chemistry” from the University of Guizhou in 2012. In 2013, he worked as a lecturer at the School of Pharmaceutical Engineering of Guizhou Institute of Technology. In 2016, he started his PhD titled “Novel Multivalent Molecules as Antibiofilm and Antibacterial Agents” at the University of Namur under the supervision of Professor Stéphane VINCENT in the research unit of Organic and Bio-organic Supramolecular Chemistry.
Abstract:
The accelerated drug resistance of bacteria is one of the most serious problems in global healthcare and the difficulties in finding new antibiotic drugs are even more challenging. Almost 80% of bacterial infections of living tissues are associated with bacterial biofilms, including lung infections of cystic fibrosis patients, colitis, urethritis, conjunctivitis, otitis, endocarditis and periodontitis.[1] Multivalency is ubiquitous in biological interactions, especially in carbohydrate-mediated processes. The low affinity of carbohydrate-mediated interactions is compensated by clustering of the ligands.[2,3] However, in real biological systems, the interfaces are usually not flat, which exhibit distinct size-features from microns (e.g., cell membranes) or sub-micron (e.g., organelles or vesicles) to several nanometers (e.g., proteins, micelles). theoretical investigation indicated the size may have great influence on folding of proteins adsorbed on nanoparticles.[4] At the same time, gold nanoparticles have interesting characteristics including a three-dimensional (3D) polyvalent carbohydrate network, a globular shape and a chemically well-defined composition.In this project, we have designed novel multivalent gold nanoparticles with functionalized fullerene-C60, to investigate size-effect of inhibition of bacterial biofilms by the gold nanoparticle conjugates
Biography:
Abstract:
Biography:
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- One-Pot Sequential Synthesis of Quinazolin-8-ol derivatives employing Heterogeneous Catalyst for Suzuki-Miyaura coupling
Session Introduction
Vijay Kumar Sharma a
PhD from Amity University Uttar Pradesh,Noida, India
Title: One-Pot Sequential Synthesis of Quinazolin-8-ol derivatives employing Heterogeneous Catalyst for Suzuki-Miyaura coupling
Biography:
Vijay Kumar Sharma is pursuing his PhD from Amity University Uttar Pradesh, Sector-125, Noida, India. He has done M.Sc. in Pharmaceutical Chemistry from Guru Nanak Dev University Amrtisar, India in 2007. He is working as Senior Research Scientist in Integral Bio Sciences Pvt. Ltd, Noida, Indiap-a drug discover incubator. He has worked as synthetic chemist for project in drug discovery for various collaborators and involved in synthesis of novel scaffolds on mg to gram scale. He has a experience of over 12 years in this area and worked with premier organization such as Ranbaxy Laboratories, Gurugram, India. (now Sun Pharmaceutical Industries Limited) and Jubilant Chemsys Limited Noida, India
Abstract:
Quinazolines are pivotal heterocycles in medicinal chemistry. These have been isolated from different plants and microorganisms and are often the central core of complex natural products such as farinamycin [1], phaitanthrin C and methylisatoid [2] etc. (Figure 1) which have various biological Further, many synthetic quinazoline derivatives such as batracyclin for its anti-tumor activity [5], and the piperazine-containing trimazosin and prazosin for the treatment of high blood pressure, symptoms of an enlarged prostate, post-traumatic stress disorder (PTSD) and preventing neurodegenerative diseases such as Parkinson’s disease (PD All of these derivatives have been synthesized by multistep reactions with low to moderate yields.We have reported an efficient and eco-friendly method for a one-pot sequential synthesis of quinazolin-8-ol derivatives. A variety of boronic acids were used for Suzuki-Miyaura coupling with commercially-available SiliaCat®DPP-Pd heterogeneous catalyst. Use of this catalyst ensures minimal leaching of palladium in the product and alleviates the need of further purification. The reaction conditions used in the four synthetic steps were optimized to telescope three intermediates without first requiring their isolation to establish an efficient and eco-friendly one-pot synthesis Significance, synthetic strategy, experimental details and characterization of these newly developed interesting molecules
Tao Wang
Master`s degree in “Medicinal Chemistryâ€University of Guizhou
Title: Novel Multivalent Glyco-gold Nanoparticles to Inhibit Bacterial Fim H
Biography:
Tao WANG received his Master`s degree in “Medicinal Chemistry” from the University of Guizhou in 2012. In 2013, he worked as a lecturer at the School of Pharmaceutical Engineering of Guizhou Institute of Technology. In 2016, he started his PhD titled “Novel Multivalent Molecules as Antibiofilm and Antibacterial Agents” at the University of Namur under the supervision of Professor Stéphane VINCENT in the research unit of Organic and Bio-organic Supramolecular Chemistry.
Abstract:
The accelerated drug resistance of bacteria is one of the most serious problems in global healthcare and the difficulties in finding new antibiotic drugs are even more challenging. Almost 80% of bacterial infections of living tissues are associated with bacterial biofilms, including lung infections of cystic fibrosis patients, colitis, urethritis, conjunctivitis, otitis, endocarditis and periodontitis.[1] Multivalency is ubiquitous in biological interactions, especially in carbohydrate-mediated processes. The low affinity of carbohydrate-mediated interactions is compensated by clustering of the ligands.[2,3] However, in real biological systems, the interfaces are usually not flat, which exhibit distinct size-features from microns (e.g., cell membranes) or sub-micron (e.g., organelles or vesicles) to several nanometers (e.g., proteins, micelles). theoretical investigation indicated the size may have great influence on folding of proteins adsorbed on nanoparticles.[4] At the same time, gold nanoparticles have interesting characteristics including a three-dimensional (3D) polyvalent carbohydrate network, a globular shape and a chemically well-defined composition.
In this project, we have designed novel multivalent gold nanoparticles with functionalized fullerene-C60, to investigate size-effect of inhibition of bacterial biofilms by the gold nanoparticle conjugates.