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Synthesis and Comparative Study of Anti‐ Mycobacterium Activity of a Novel Series of Fluoronitrobenzothiazolopyrazoline Regioisomers
Author(s) -
Hazra K.,
Nargund L. V. G.,
Rashmi P.,
Narendra Sharath Chandra J. N.,
Nandha B.,
Harish M. S.
Publication year - 2012
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201100072
Subject(s) - cytotoxicity , mycobacterium tuberculosis , stereochemistry , benzothiazole , chemistry , strain (injury) , in vitro , ring (chemistry) , antibacterial activity , tuberculosis , biology , biochemistry , bacteria , medicine , organic chemistry , genetics , pathology , anatomy
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.

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