Editor-in-Chief Hatice Kübra Elçioğlu Vice Editors Levent Kabasakal Esra Tatar Online ISSN 2630-6344 Publisher Marmara University Frequency Bimonthly (Six issues / year) Abbreviation J.Res.Pharm. Former Name Marmara Pharmaceutical Journal
Journal of Research in Pharmacy 2023 , Vol 27 , Issue 1
Design and synthesis of novel lactam/thiazole derivatives having five membered thiazolyl ring and their antimicrobial activity
Krishna SRIVASTAVA1,Ram Prakash TIWARI1,Raj Bahadur SINGH1,Abhishek SRIVASTAVA2,Deepa LAKHMANI1,Rishi Kumar VISHNOI3
1Faculty of Chemical Sciences, Shri Ramswaroop Memorial University (SRMU), Barabanki. 225 003, U.P. (India)
2Department of Chemistry, GLA University, Mathura, 281006, U.P. (India)
3Department of Chemistry University of Lucknow, Lucknow 226007 U.P. (India)
DOI : 10.29228/jrp.308 In the present communication, we conceived a new synthetic approach for the preparation of novel thiazolyl-lactam/thiazole analogs. The reaction was started through cyclization of ketone with thiourea along with substituted aryl aldehydes to culminate imine derivatives which subsequently cyclized with thioglycolic acid/chloroacetyl chloride to produce final compounds. The structural elucidation of newly synthesized compounds was performed through elemental detections, FT-IR, 1HNMR, and Mass spectrometric techniques. Antimicrobial studies were performed for all synthesized molecules by serial dilution method by tacking the positive (K. pneumonia, S. aureus, B. subtills) and negative (P. aeruginosa and E. coli.) bacterial strains. The in vitro antimicrobial screening results show that the compounds 2e, 3c, and 3d containing o-hydroxy, p-chloro, and p-nitro substituent respectively exhibit exceptional activity against S. aureus while compounds 2d and 3f bearing p-nitro and o-chloro substituent respectively were deemed to be the most competent against B. subtilis. Compounds 2d (p-nitro) and 2f (o-chloro) were found to be most potent against E. coli. In gram-negative bacterial strains, compounds 2c (p-chloro), 2g (4-OH,-OCH3), 3b (p-hydroxy), and 3e (o-hydroxy) were extremely potent against P. aeruginosa while compound 2e containing o-hydroxy group shows excellent activity against E.coli. Keywords : Synthesis; Lactam; Thiazolyl ring; Antimicrobial activity; Thiourea
Marmara University