NOVEL UREA AND THIOUREA DERIVATIVES OF THIAZOLE-GLUTAMIC ACID CONJUGATE AS POTENTIAL INHIBITORS OF MICROBES AND FUNGI

© 2013 A. Sharma, R. Suhas, S. Chandan, D. Ch. Gowda^#

^#Phone: +91 821 2419664; e-mail: dchannegowda@yahoo.co.in

Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570006, Karnataka, India

Received March 21, 2013; in final form, April 17, 2013

Since discovery and development of effective as well as safe drugs has brought a progressive era in human healthcare that is accompanied by the appearance of drug resistant bacterial strains, there is constant need of new antibacterial agent having novel mechanisms of action to act against the harmful pathogens. In the present study, several N-terminal substituted urea/thiourea derivatives were synthesized by the reaction of glutamic acid and 3-(1-piperazinyl)-1,2-benzisothiazole with various substituted phenyl isocyanates/isothiocyanates. Elemental analysis, IR, ¹H NMR, ¹³C NMR and mass spectral data confirmed the structure of the newly synthesized compounds. The derivatives were investigated for their antibacterial and antifungal activities against various pathogens of human origin by agar well diffusion method and microdilution method. The preliminary antimicrobial bioassay reveals that the compounds containing fluoro and bromo as substituents showed promising antimicrobial activity.

Keywords: glutamic acid, thiazole, conjugation, urea/thiourea, antimicrobial

Биоорг. химия 2013, 39 (6): 736-744