SYNTHESIS, CHARACTERIZATION AND ANTIBACTERIAL EVALUATION OF NOVEL Β- LACTAM AND THIAZOLIDIN-4-ONE DERIVATIVES HAVING THIADIAZINYL RING
Srivastava, K., Prakash, R., Singh, R., Srivastava, A., Vishnoi, R. (2023). SYNTHESIS, CHARACTERIZATION AND ANTIBACTERIAL EVALUATION OF NOVEL Β- LACTAM AND THIAZOLIDIN-4-ONE DERIVATIVES HAVING THIADIAZINYL RING. EKB Journal Management System, 46(1), 203-216. doi: 10.21608/bfsa.2023.300922
Krishna Srivastava; Ram Prakash; Raj Bahadur Singh; Abhishek Srivastava; Rishi kumar Vishnoi. "SYNTHESIS, CHARACTERIZATION AND ANTIBACTERIAL EVALUATION OF NOVEL Β- LACTAM AND THIAZOLIDIN-4-ONE DERIVATIVES HAVING THIADIAZINYL RING". EKB Journal Management System, 46, 1, 2023, 203-216. doi: 10.21608/bfsa.2023.300922
Srivastava, K., Prakash, R., Singh, R., Srivastava, A., Vishnoi, R. (2023). 'SYNTHESIS, CHARACTERIZATION AND ANTIBACTERIAL EVALUATION OF NOVEL Β- LACTAM AND THIAZOLIDIN-4-ONE DERIVATIVES HAVING THIADIAZINYL RING', EKB Journal Management System, 46(1), pp. 203-216. doi: 10.21608/bfsa.2023.300922
Srivastava, K., Prakash, R., Singh, R., Srivastava, A., Vishnoi, R. SYNTHESIS, CHARACTERIZATION AND ANTIBACTERIAL EVALUATION OF NOVEL Β- LACTAM AND THIAZOLIDIN-4-ONE DERIVATIVES HAVING THIADIAZINYL RING. EKB Journal Management System, 2023; 46(1): 203-216. doi: 10.21608/bfsa.2023.300922

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

Bulletin of Pharmaceutical Sciences Assiut University
Volume 46, Issue 1, June 2023, Page 203-216  XML PDF (1.01 MB)
Document Type: Original Article
DOI: 10.21608/bfsa.2023.300922
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Authors
Krishna Srivastava email 1; Ram Prakash1; Raj Bahadur Singh1; Abhishek Srivastava2; Rishi kumar Vishnoi3
1Department of Chemistry, Shri Ramswaroop Memorial University, Barabanki, 222502, U.P., India
2Department of Chemistry, GLA University, Mathura 281406, U.P., India
3Department 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
Keywords
Thioglycoolic acid; Thiourea; thiosemicarbazide; Cyclohexanone; Substituted Aromatic aldehyde
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