Synthesis of thiazole-phenylacetic acid compounds as dual antibacterial-COX enzymes inhibitors

Abstract

Purpose: Present a new potential dual drug for patient suffering both inflammation and infection was aim of this study therefore investigation of anti-inflammatory and antimicrobial activity of new thiazole-phenylacetic acid compounds derivatives as a potential dual drug was carried out. Materials and Methods: Anti-inflammatory activity of new synthesize drugs were determined via fluorometric assay. Assay based on fluorometric detection of intermediates prostaglandin G1 and G2 during COX1 (cyclooxygenases-1) and COX2 (cyclooxygenases- 2) enzyme inhibition, respectively. Ibuprofen and Nimesulide were used as reference drugs. Antimicrobial activity of compounds in parallel were evaluated with microbroth dilution assay. Two-fold serial dilution of compounds were tested against microorganisms and minimum inhibition concentration of compound were determined according to CLSI (Clinical and Laboratory Standards Institute). Chloramphenicol was used as a control drug. Results: Fluorometric assay and antimicrobial assay results were compared. The observation was compound 2b had important inhibitory activity on COX1 and COX2 but activity of 2d carrying 4-chlorophenyl and phenyl was more successful than 2b and also antimicrobial activity of 2d against microorganism was better or same as reference drug chloramphenicol. Conclusion: Between the new synthesized compound, 2d exhibited remarkable anti-inflammatory and antibacterial activity. 2d can be evaluated as a promising drug potential. Further investigation on scaffold of 2d will help to develop new alternatives for dual anti-inflammatory and antibacterial agent which can provide relief for patients in suffering from the symptoms of these diseases.