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