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Synthesis, evaluation and molecular docking studies of amino acid derived N-glycoconjugates as antibacterial agents.

Abstract：

:Six 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.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Baig N,Singh RP,Chander S,Jha PN,Murugesan S,Sah AK

doi

10.1016/j.bioorg.2015.10.002

subject

Has Abstract

pub_date

2015-12-01 00:00:00

pages

110-5

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(15)30026-2

journal_volume

63

pub_type

杂志文章

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