DESIGN, SYNTHESIS, AND PHARMACOLOGICAL EVALUATION OF SOME NOVEL BIS-THIAZOLE DERIVATIVES

• Published in: Asian journal of pharmaceutical and clinical research 2018-04, Vol.11 (4), p.164
• Main Authors: Borde, Ramesh M, B Jadhav, Satish, R Dhavse, Rahul, S Munde, Achut
• Format: Article
• Language: English
• ISSN: 0974-2441; 0974-2441
• DOI: 10.22159/ajpcr.2018.v11i4.23413

 Objective: A series of substituted 5,2-bis-thiazoles derivatives were synthesized by Hantzsch reaction and evaluated in vitro for antimicrobial activity against Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, and Staphylococcus aureus. Methods: 2-(4-(benzyloxy)phenyl)-4-methylthiazole-5-carbothioamide were synthesized and allowed to react with various α-haloketones to give 5,2-bis-thiazoles, i.e., 2-(4-(benzyloxy)phenyl)-4-methyl-5-(4-substituted thiazol-2-yl)thiazole derivatives in excellent yield. The synthesized compounds were characterized by spectroscopic methods as well as elemental analyses. They were screened for their antimicrobial activity using the agar diffusion method.Result: Literature survey reveals that the synthesis of 2-(4-(benzyloxy)phenyl)-4-methyl-5-(4-substituted thiazol-2-yl)thiazole, i.e., (5,2-Bis-thiazoles) derivatives (10a-e) was not reported. The entire compound exhibited mild to moderate antimicrobial activity.Conclusion: The antimicrobial results revealed that the synthesized derivatives have significant antimicrobial properties, and further, structure– activity relationship studies may develop more potent and less toxic molecule.