Coumarin-benzimidazole hybrids as a potent antimicrobial agent: synthesis and biological elevation

Molecular hybridization approach is an emerging tool in drug discovery for designing new pharmacophores with biological activity. A novel, new series of coumarin-benzimidazole hybrids were designed, synthesized and evaluated for their broad spectrum antimicrobial activity. Among all the synthesized...

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Bibliographic Details
Published in:Journal of antibiotics 2017-09, Vol.70 (9), p.954-961
Main Authors: Singh, L Ravithej, Avula, Srinivasa Rao, Raj, Sneha, Srivastava, Akanksha, Palnati, Gopala Reddy, Tripathi, C K M, Pasupuleti, Mukesh, Sashidhara, Koneni V
Format: Article
Language:English
Subjects:
Animals
Anti-Bacterial Agents - adverse effects
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacology
Anti-Infective Agents - adverse effects
Anti-Infective Agents - chemical synthesis
Anti-Infective Agents - chemistry
Anti-Infective Agents - pharmacology
Antibacterial activity
Antimicrobial activity
Antimicrobial agents
Bacillus subtilis - drug effects
Bacillus subtilis - growth & development
Benzimidazoles
Benzimidazoles - adverse effects
Benzimidazoles - chemical synthesis
Benzimidazoles - chemistry
Benzimidazoles - pharmacology
Biological activity
Cell Line
Cell Survival - drug effects
Chemical synthesis
Chlorine
Connective Tissue Cells - cytology
Connective Tissue Cells - drug effects
Coumarin
Coumarins - adverse effects
Coumarins - chemical synthesis
Coumarins - chemistry
Coumarins - pharmacology
Cytotoxicity
Drug Design
Drug Resistance, Multiple, Bacterial
Hemolysis - drug effects
Humans
Hybridization
Hybrids
Hydrocarbons, Chlorinated - adverse effects
Hydrocarbons, Chlorinated - chemical synthesis
Hydrocarbons, Chlorinated - chemistry
Hydrocarbons, Chlorinated - pharmacology
Mice
Microbial Sensitivity Tests
Minimum inhibitory concentration
Models, Molecular
Molecular Structure
Pharmacophores
Proteus vulgaris - drug effects
Proteus vulgaris - growth & development
Pseudomonas aeruginosa
Pseudomonas aeruginosa - drug effects
Pseudomonas aeruginosa - growth & development
Staphylococcus aureus - drug effects
Staphylococcus aureus - growth & development
Stereoisomerism
Structure-Activity Relationship
Toxicity
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Summary:Molecular hybridization approach is an emerging tool in drug discovery for designing new pharmacophores with biological activity. A novel, new series of coumarin-benzimidazole hybrids were designed, synthesized and evaluated for their broad spectrum antimicrobial activity. Among all the synthesized molecules, compound (E)-3-(2-1H-benzo[d]imidazol-1-yl)-1-((4-chlorobenzyl)oxy)imino)ethyl)-2H-chromen-2-one showed the most promising broad spectrum antibacterial activity against Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis and Proteus vulgaris. In addition, it has showed no cytotoxicity and hemolysis at 10 times the MIC concentration. SAR studies indicate that position of the chlorine atom in the hybrid critically determines the antibacterial activity.
ISSN:0021-8820
1881-1469
DOI:10.1038/ja.2017.70