title: Synthesis, antimicrobial evaluation and QSAR studies of 2-chlorobenzoic acid derivatives.
abstract: In the present study, 2-chlorobenzoic acid derivatives were synthesized and evaluated for their antimicrobial activity against Gram-positive bacteria: Staphylococcus aureus, Bascillus subtilis, Gram-negative bacterium Escherichia coli, fungal strains: Candida albicans and Aspergillus niger by tube dilution method. Results of antimicrobial screening indicated that the synthesized compounds exhibited greater antibacterial potential against Gram-negative bacterium (Escherichia coli) than Gram-positive bacteria and the Schiff's bases of 2-chloro benzoic acid were more potent antimicrobial agents than its esters. Compound 6 (pMIC(am)=1.91 µM/ml, pMIC(ec)=2.27 µM/ml) emerged as most potent antimicrobial agent and was found comparable to standard drug norfloxacin (pMIC(ec)=2.61 µM/ml) against Escherichia coli. QSAR studies revealed that the antibacterial, antifungal and the overall antimicrobial activities of the 2-chlorobenzoic acid derivatives were governed by the topological parameters, second order and valence second order molecular connectivity indices ((2)χ and (2)χ(v)).
authors.affiliation: Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, India.
authors.forename: S
authors.initials: S
authors.lastname: Mehta
authors.affiliation: Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, India.
authors.forename: P
authors.initials: P
authors.lastname: Kumar
authors.affiliation: Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, India.
authors.forename: R K
authors.initials: RK
authors.lastname: Marwaha
authors.affiliation: Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, India.
authors.forename: B
authors.initials: B
authors.lastname: Narasimhan
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002723:Chlorobenzoates / Q000138:chemical synthesis* / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D021281:Quantitative Structure-Activity Relationship
chemical_list: D000890:Anti-Infective Agents; D002723:Chlorobenzoates