A robust synthesis of functionalized 2 H -indazoles via solid state melt reaction (SSMR) and their anti-tubercular activity

Vidyacharan, Shinde and Adhikari, Chandan and Sharada, D S and Reshma, Rudraraju Srilakshmi et. al. (2017) A robust synthesis of functionalized 2 H -indazoles via solid state melt reaction (SSMR) and their anti-tubercular activity. Bioorganic & Medicinal Chemistry Letters, 27 (7). pp. 1593-1597. ISSN 0960894X

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Abstract

A facile and convenient approach has been developed for the synthesis of functionalized indazoles via solid state melt reaction using easily accessible starting materials under catalyst-free conditions. This transformation involves electrocyclization via a conjugated nitrene intermediate obtained under thermal conditions. Further anti-tubercular activity screening of the molecules was undertaken, among the compounds 3a-3x screened for in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv, compound 3u (MIC: 4.20 μM) was found to be most active and are superior over existing standard drugs ciprofloxacin and ethambutol. Compounds 3c and 3x were found to equally potent as ethambutol. Among most potent compounds in the series, four compounds (3n, 3o, 3p and 3u) showed lower cytotoxicity which could be promising drug candidates for further development.

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