Synthesis and Comparative Study of Anti-Mycobacterium Activity of a Novel Series of Fluoronitrobenzothiazolopyrazoline Regioisomers

✍ Scribed by K. Hazra; L. V. G. Nargund; P. Rashmi; J. N. Narendra Sharath Chandra; B. Nandha; M. S. Harish

• Publisher: John Wiley and Sons
• Year: 2011
• Tongue: English
• Weight: 211 KB
• Volume: 345
• Category: Article
• ISSN: 0365-6233
• DOI: 10.1002/ardp.201100072

✦ Synopsis

Abstract

In an attempt to find a new and a safer drug for tuberculosis, we have synthesized a series of fluoronitrobenzothiazolopyrazolines for antitubercular activity. The series comprises three subclasses: fluorobenzothiazolopyrazolines (11a–f), fluoronitrobenzothiazolopyrazoline, nitro group at 5^th^ position (12a–f) and 4^th^ position (13a–f). All compounds were screened for their in‐vitro antitubercular activity against Mycobacterium tuberculosis H37Rv strain by using Middlebrook 7H‐9 broth. An introduction of NO~2~ group at 5^th^ position of benzothiazole ring (12a–f) increased the antitubercular activity whereas introduction of NO~2~ group at 4^th^ position (13a–f) was found to decrease the activity remarkably. Two compounds from each series showing good antitubercular activity were tested for cytotoxicity on THP‐1 cell lines and they showed low cytotoxicity.