5(4H)‐Oxazolones as Novel Antitubercular Agents: Synthesis,Characterisation and Structure Activity Study |
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| Authors: | K P Suhasini Praveen K Chintakindi K Chaguruswamy Y L N Murthy |
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| Institution: | 1. Dept. of Organic Chemistry, Andhra University, Visakhapatnam, Andhra Pradesh, India;2. Vignan Institute of Engineering for Women, Visakhapatnam, Andhra Pradesh, India;3. Bio‐Organic Chemistry Division, Indian Institute of Integrative Medicine (IIIM), Jammu, India;4. Catalysis and Peptide Research Unit, University of KwaZulu‐Natal, Durban, South Africa |
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| Abstract: | In search of novel anti tubercular agents, a series of twelve 4‐(substituted benzylidene)‐2‐p‐tolyloxazol‐5(4H)‐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. |
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| Keywords: | 5(4H)‐Oxazolones Erlenmeyer‐Plochl azlactone synthesis 4A0 molecular sieves Antitubercular M tuberculosis H37Rv Rifampicin Isoniazid |
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