BITS Faculty Publications
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Item Quinoline Glycoconjugates as Potentially Anticancer and Anti-Inflammatory Agents: An Investigation Involving Synthesis, Biological Screening, and Dockin(ECSP, 2020-08-20) Dubey, Uma S.; Sah, Ajay Kumar; Shukla, ParitoshThe present work is a preliminary report of synthesis of a series of targeted 4,6-O-ethylidene-β-D-glucopyranosylamine glycoconjugate quinoline 4-carboxylic acid derivatives followed by a quick evaluation of their anti-inflammatory and anticancer activities. Compounds C5 and C8 exhibited highest anti-inflammatory activity against human COX-2 enzyme. Anticancer studies were also performed in vitro which revealed C8 as a promising candidate against HeLa, human cervical cancer cell lines. The anti-inflammatory and anticancer activity was further confirmed by molecular docking studies for all the synthesized molecules. That all the compounds showed potency, seems to validate our initial hypothesis concerning a positive correlation between anticancer and anti-inflammatory activity for the designed quinoline glycoconjugates.Item Synthesis, evaluation and molecular docking studies of amino acid derived N-glycoconjugates as antibacterial agents(Elsiever, 2015-12) Jha, Prabhat N.; Sah, Ajay Kumar; Murugesan, SankaranarayananSix amino acid derived N-glycoconjugates of d-glucose were synthesized, characterized and tested for antibacterial activity against G(+)ve (Bacillus cereus) as well as G(−)ve (Escherichia coli and Klebsiella pneumoniae) bacterial strains. All the tested compounds exhibited moderate to good antibacterial activity against these bacterial strains. The results were compared with the antibacterial activity of standard drug Chloramphenicol, where results of A5 (Tryptophan derived glycoconjugates) against E. coli and A4 (Isoleucine derived glycoconjugates) against K. pneumoniae bacterial strains are comparable with the standard drug molecule. In silico docking studies were also performed in order to understand the mode of action and binding interactions of these molecules. The docking studies revealed that, occupation of compound A5 at the ATP binding site of subunit GyrB (DNA gyrase, PDB ID: 3TTZ) via hydrophobic and hydrogen bonding interactions may be the reason for its significant in vitro antibacterial activity.Item Synthesis of Glucose-Derived Glycoconjugates and Studies on Their Antimicrobial Activities: Mechanistic Insight(Wiley, 2016-10) Jha, Prabhat N.; Sah, Ajay KumarThree N-glycoconjugates have been condensed with four aromatic aldehydes to afford imine linkage containing twelve new compounds. These compounds were tested for antibacterial activity against three bacteria [gram positive (Bacillus cereus) and gram negative (Escherichia coli and Klebsiella pneumoniae)] and antifungal activity against Fusarium graminearum, Fusarium monilliforme and Aspergillus flavus. All the compounds exhibited fair amount of antibacterial activities against both types of bacteria, but antifungal activity was exhibited by only three compounds, which contained naphthyl moiety. Microbial cell penetration ability of two most efficient compounds and discrimination of live/dead cells have been explored using microscopic technique. Effect of these two compounds on bacterial nucleic acids have also been studied, which helped in understanding the mechanistic insights of cell death.