Novel Armed Pyrazolobenzothiazine Derivatives: Synthesis, X-Ray Crystal Structure and POM analyses of Biological Activity Against Drug Resistant Clinical Isolate of Staphylococcus aureus

• Published in: Pharmaceutical Chemistry Journal
• Main Author: Sajid Z.; Ahmad M.; Aslam S.; Ashfaq U.A.; Zahoor A.F.; Saddique F.A.; Parvez M.; Hameed A.; Sultan S.; Zgou H.; Hadda T.B.
• Format: Article
• Language: English
• Published: Springer New York LLC 2016
• Online Access: https://www.scopus.com/inward/record.uri?eid=2-s2.0-84978039210&doi=10.1007%2fs11094-016-1417-y&partnerID=40&md5=05562b99750bceb52c0d1899413d8241
• ISSN: 0091150X
• DOI: 10.1007/s11094-016-1417-y

Novel structural hybrids of pyrazolobenzothiazine and triazole ring systems have been prepared to observe a synergistic effect of the two ring systems. The methodology involves condensation of pyrazolobenzothiazine rings with methyl chloroacetate, followed by hydrazide formation. The hydrazides were converted to triazoles through the formation of intermediate potassium salts of dithiocarbazate. The final compounds as well as intermediates were screened for their antibacterial activity against a multidrug resistant strain of Staphylococcus aureus. It was interesting to observe that dithiocarbazates (7a, 7b) and target triazoles (8a, 8b) exhibited antibacterial activity. © 2016, Springer Science+Business Media New York.