Abstract

ANTI-INFLAMMATORY, ANTIMICROBIAL ACTIVITY AND QSAR STUDIES OF ANTHRANILIC ACID DERIVATIVES

*Meenu Beniwal, Viney Lather, Vikramjeet Judge, Neelam Jain, Amit Beniwal 

ABSTRACT

Almost all the major classes of antibiotics have encountered resistance in clinical applications. The emergence of bacterial resistance to β-lactam antibiotics, macroliodes, quinolones and vancomycin is becoming a major worldwide health problem. The increasing incidence of bacterial resistance to established antibiotic classes is driving researchers to search for newer antibacterial agents. The anthranilic acid is a constituent of many of the bioactive compounds that exhibits a range of biological activities. Specifically, the nucleus of anthranilic acid is the biochemical precursor of amino acid and its derivatives as well as constituents of alkaloids. Moreover, the anthranilic acid derivatives have been found to possess good anti inflammatory activity. The present work was undertaken to develop some newer antimicrobial and anti-inflammatory agents based on anthranilic acid and QSAR studies were performed to relate their antimicrobial activity with their structure. The results of anti-inflammatory activity indicated that 5-chloro-2-[3-(4-chloro-phenylsulfamoyl)-benzoylamino]-benzoic acid exhibited the highest percentage inhibition of paw oedema which was higher than standard drug Ibuprofen. The results of antimicrobial activity pointed out that (2-[3-(3-phenylsulfamoyl-phenyl)-acryloylamino]-benzoic acid) and (2-[3-(3-ethylsulfamoyl-phenyl)-acryloylamino]-benzoic acid) have appreciable antimicrobial and antifungal activities. The QSAR studies revealed the fact that the antimicrobial activity of anthranilic acid derivatives was governed by topological descriptors.

Keywords: Anthranilic acid; antimicrobial activity; anti-inflammatory activity; QSAR.