Abstract

SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL 1, 3 THIAZOLE DERIVATIVES

Lambe Sujata Vitthal* and Ghogare Pradip Babasaheb

Abstract

Aim: Synthesis and biological evaluation of novel 1, 3 thiazole derivatives. Materials and Methods: Thin-layer chromatography plates used for final recrystallized product were pre-coated silica gel G plates. Solvent systems were developed using trial and error method by the use of appropriate solvents of different polarity. Fourier transform infrared spectra (FTIR) were recorded using FTIR 8400 FShimadzu spectrometer using KBr disc pellet method. 1H nuclear magnetic resonance (NMR) spectra of synthesized compounds were recorded on “BRUKER AVANCE II 400” NMR spectrometer at 400 MHz frequency in dimethyl sulfoxide using tetramethylsilane as internal standard (chemical shift values expressed in delta ppm). Synthesis of ethyl 2-amino-4-methylthiazole- 5-carboxylate, synthesis of ethyl 2-(arylidine amino)-4-methylthiazole-5-carboxylate, and synthesis of ethyl 2-(3- chloro-2-(arylidine)-4 oxazetidine -1-yl)-4-methylthiazole-5-carboxylate. Results and Discussion: In the present work, a new series of Schiff bases were synthesized from ethyl 2-amino-4-methyl thiazole5 carboxylate with substituted aromatic aldehydes in the presence of catalytic amount of benzoyl peroxide. The resulted Schiff bases undergoes cyclocondensation reaction with chloroacetyl chloride in the presence of triethylamine under cold conditions will yield the title compounds. Conclusion: The new compounds were screened for their antibacterial and antifungal activity. In the antibacterial activity, a compound 3c has shown maximum activity against all the four pathogenic micro-organisms.

Keywords: 1, 3 thiazole, antibacterial and antifungal activity, aryl dine derivatives.