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5(4 H )‐Oxazolones as Novel Antitubercular Agents: Synthesis, Characterisation and Structure Activity Study
Author(s) -
Suhasini K. P.,
Chintakindi Praveen K.,
Chaguruswamy K.,
Murthy Y. L. N.
Publication year - 2015
Publication title -
journal of the chinese chemical society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.329
H-Index - 45
eISSN - 2192-6549
pISSN - 0009-4536
DOI - 10.1002/jccs.201500111
Subject(s) - chemistry , rifampicin , isoniazid , mycobacterium tuberculosis , stereochemistry , in vitro , tuberculosis , molecule , combinatorial chemistry , antibiotics , organic chemistry , biochemistry , pathology , medicine
In search of novel anti tubercular agents, a series of twelve 4‐(substituted benzylidene)‐2‐ p ‐tolyloxazol‐5(4 H )‐ones (5a – 5l) has been synthesized, characterised and subjected to evaluate their antitubercular activity for the first time against Mycobacterium tuberculosis H37Rv (ATCC 27294). The out‐put of these studies disclosed that all the synthesized target molecules of the series displayed good to moderate activity with MIC values ranging 2–32 μg/mL in comparison with the standard first line antitubercular drugs Rifampicin and Isoniazid. Compound 5e with three methoxy groups meta to each other, is the most distinctive compound identified amongst the series, because of its remarkable in vitro antitubercular activity and thus may act as a promising lead molecule for further explorations.