SYNTHESIS, CHARACTERIZATION AND ANTIBACTERIAL EVALUATION OF NOVEL Β- LACTAM AND THIAZOLIDIN-4-ONE DERIVATIVES HAVING THIADIAZINYL RING

Document Type : Original Article

Authors

1 Department of Chemistry, Shri Ramswaroop Memorial University, Barabanki, 222502, U.P., India

2 Department of Chemistry, GLA University, Mathura 281406, U.P., India

3 Department of Chemistry, Lucknow University, Lucknow, 226007, U.P., India

Abstract

Since ancient times, several heterocyclic scaffolds have been recognized as possessing a wide spectrum of anti-infectious pharmacological properties. The present work aimed to synthesize and to perform antibacterial screening of some novel heterocyclic derivatives of thiadiazinyl β-lactam and thiazolidin-4-one. Cyclization of thiosemicarbazide with cyclohexanone and substituted aromatic aldehydes leads to the formation of Schiff bases, which form thiazolidinone derivatives upon reaction with thioglycolic acid in the presence of a catalytic amount of ZnCl2. Lactam derivatives were synthesized by the cyclization of Schiff bases with chloroacetyl chloride in presence of triethyl amine. The synthesized derivatives 2a (MIC 25 µg/ml), and 3f (MIC 25 µg/ml) with 4-OH, 3-OCH3, and o-hydroxy substituents, respectively, exhibit good activity against S. aureus, while compound 2c containing p-nitro substituent was found to be the most active (MIC 12.5 µg/ml) against B. subtilis. In Gram-negative bacterial strains, compound 3b (o-chloro) was extremely potent (MIC 12.5 µg/ml) against P. pneumonia while compound 2d containing the p-hydroxy group shows excellent activity (MIC 12.5 µg/ml) against E.coli

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