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Synthesis, biological screening and molecular modeling studies of novel 3-chloro-4-substituted-1-(2-(1H-benzimidazol-2-yl)phenyl))-azetidin-2-ones.

Authors :
Chhajed SS
Upasani CD
Source :
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2012 Aug; Vol. 27 (4), pp. 504-8. Date of Electronic Publication: 2011 Aug 08.
Publication Year :
2012

Abstract

In the present investigation synthesis of some novel 1-(2-(1H-benzimidazol-2-yl)phenyl)-3-chloro-4-(Un/substitutedphenyl)azetidin-2-one (3a-3h) antibacterial are reported. Structures of synthesized compounds were confirmed by spectral techniques (IR, Mass, (1)H-NMR) All reactions were monitored with analytical thin layer chromatography. Synthesized compounds were docked in to the active site of enzyme transpeptidase. Compounds 3a, 3b, 3d and 3g were found to have good affinity for transpeptidase with potent antibacterial activity. A good correlation is found between in silico docking analysis and in vitro antibacterial activity.

Details

Language :
English
ISSN :
1475-6374
Volume :
27
Issue :
4
Database :
MEDLINE
Journal :
Journal of enzyme inhibition and medicinal chemistry
Publication Type :
Academic Journal
Accession number :
21823835
Full Text :
https://doi.org/10.3109/14756366.2011.598867