Substituted 3-((Z)-2-(4-nitrophenyl)-2-(lH-tetrazol-5-yl) vinyl)-4H-chromen-4-ones as novel anti-MRSA agents : Synthesis, SAR, and in-vitro assessment

In search for a new antibacterial agent with improved antimicrobial spectrum and potency, we designed and synthesized a series of novel 3-((Z)-2-(4-nitrophenyl)-2-(1H-tetrazol-5-yl) vinyl)-4H-chromen-4-ones 7a-h by convergent synthesis approach. All the synthesized compounds were assayed for their i...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2008-08, Vol.18 (16), p.4678-4681
Main Authors: DIWAKAR, Santosh D, BHAGWAT, Sachin S, SHINGARE, Murlidhar S, GILL, Charansing H
Format: Article
Language:English
Subjects:
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - pharmacology
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Biological and medical sciences
Carboxylic Acids - chemistry
Chemistry, Pharmaceutical - methods
Chromones - chemical synthesis
Chromones - pharmacology
Drug Design
Escherichia coli
Escherichia coli - metabolism
Humans
Medical sciences
Methicillin Resistance - drug effects
Microbial Sensitivity Tests
Models, Chemical
Molecular Structure
Pharmacology. Drug treatments
Staphylococcus aureus
Staphylococcus aureus - drug effects
Streptococcus pneumoniae
Structure-Activity Relationship
Tetrazoles - chemical synthesis
Tetrazoles - chemistry
Tetrazoles - pharmacology
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Summary:In search for a new antibacterial agent with improved antimicrobial spectrum and potency, we designed and synthesized a series of novel 3-((Z)-2-(4-nitrophenyl)-2-(1H-tetrazol-5-yl) vinyl)-4H-chromen-4-ones 7a-h by convergent synthesis approach. All the synthesized compounds were assayed for their in-vitro antibacterial activities against gram-negative and gram-positive bacteria. The preliminary structure-activity relationship, to elucidate the essential structure requirements for the antimicrobial activity that results into anti-MRSA (methicillin-resistant S. aureus) potential, has been described. Amongst the synthesized compounds 7d, 7e, 7f and 7h were found to possess activity against methicillin-resistant S. aureus in addition to the activity against other bacterial strains such as E. faecalis, S. pneumoniae, and E. coli.
ISSN:0960-894X
0968-0896
1464-3405
1464-3391
DOI:10.1016/j.bmcl.2008.07.007