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Drug Res (Stuttg) 2014; 64(4): 208-213
DOI: 10.1055/s-0033-1355355
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

Synthesis, Antimicrobial Evaluation and QSAR Studies of 2-chlorobenzoic Acid Derivatives

S. Mehta
1   Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, India
,
P. Kumar
1   Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, India
,
R. K. Marwaha
1   Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, India
,
B. Narasimhan
1   Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, India
› Author Affiliations
Further Information

Publication History

received 28 July 2013

accepted 23 August 2013

Publication Date:
20 November 2013 (online)

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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 (pMICam=1.91 µM/ml, pMICec=2.27 µM/ml) emerged as most potent antimicrobial agent and was found comparable to standard drug norfloxacin (pMICec=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 (2χ and 2χv).

Key words

antibacterial drugs - antifungal drugs - infectious diseases
 

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