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Pharmaceutics
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SYNTHESIS, CHARACTERIZATION OF 2-METHYLQUINOZOLINYL THIAZOLIDINES FOR ANTI-MICROBIAL ACTIVITY


Abstract

Author(s): Shivanand Kolageri*, Shiva Kumar B, Santosh Karajagi, Gaviraj E.N and Kotnal R.B.

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 goodactivity and others showed moderate to weak activity at the concentration of 250 μ/mL, 500 μ/mL and 750 μ/mL compared to Chloramphenicol drug.

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