SYNTHESIS, CHARACTERIZATION OF 2-METHYLQUINOZOLINYL THIAZOLIDINES FOR ANTIMICROBIAL ACTIVITY.

Shivanand Kolageri*, B. Shivakumar, S. M. Biradar, Santosh Karajagi and E. N. Gaviraj

ABSTRACT

Six new derivatives of 3-(4-oxo-2-arylthiazolidin-3-yl)-2-methylquinazolin-4(3H)-one were synthesized by condensation between 3-amino-2-methylquinozolin-4(3H)-one and substituted aromatic aldehydes using thioglycolic acid, N,N’-dicylohexylcarbodiimide and N,N-dimethyl formamide as solvent. The required 3-amino-2-methylquinozolin-4(3H)-one was obtained from the reaction between 2-amino benzoic acid and acetic anhydride/acetyl chloride. The synthesized compounds containing quinazoline nucleus coupled with thiazolidinone could yield effective biologically active derivatives. Hence the objectives of the research work are as synthesize newer heterocyclic derivatives of Quinazolinones with thiazolidinone, characterize the synthesized compounds using physical data like M.P, TLC and spectroscopic analysed FT-IR, 1H-NMR Spectral and these synthesized compounds were biological evaluated for their antimicrobial screening. The prepared compounds were confirmed for antibacterial activity against E. coli (gram negative) and Staphylococcus Aureus (gram positive) by using cup-plate method. The results of antibacterial activity revealed that, among all derivatives 3-[2-(2-chloroquinolin-3-yl)-4-oxo-1,3-thiazolidin-3-yl]-2-methylquinazolin-4(3H)-one showed moderate to good activity and others showed moderate to weak activity at the concentration of 250μ/ml, 500μ/ml and 750μ/ml compared to Chloramphenicol drug.

Keywords: Quinazolinones with thiazolidinone derivatives, Antibacterial activity, Cup-plate method.