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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.
- 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.
- Subjects :
- Anti-Bacterial Agents chemical synthesis
Anti-Bacterial Agents chemistry
Azetidines chemical synthesis
Azetidines chemistry
Bacillus subtilis drug effects
Benzimidazoles chemical synthesis
Benzimidazoles chemistry
Catalytic Domain drug effects
Dose-Response Relationship, Drug
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors chemistry
Escherichia coli drug effects
Microbial Sensitivity Tests
Models, Molecular
Molecular Structure
Peptidyl Transferases metabolism
Staphylococcus aureus drug effects
Structure-Activity Relationship
Anti-Bacterial Agents pharmacology
Azetidines pharmacology
Benzimidazoles pharmacology
Enzyme Inhibitors pharmacology
Peptidyl Transferases antagonists & inhibitors
Subjects
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