Synthesis and antitubercular activity of a series of hydrazone and nitrovinyl analogs derived from heterocyclic aldehydes

A series of hydrazone and 3-nitrovinyl analogs of indole-3-carboxaldehydes and related compounds were synthesized and screened for antitubercular activity against Mycobacterium tuberculosis H37RV in BACTEC 12B medium using the Microplate Alamar Blue Assay (MABA). Several compounds showed inhibitory...

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Veröffentlicht in:Journal of enzyme inhibition and medicinal chemistry 2009-02, Vol.24 (1), p.117-124
Hauptverfasser: Sonar, Vijayakumar N., Crooks, Peter A.
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Sprache:eng
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Zusammenfassung:A series of hydrazone and 3-nitrovinyl analogs of indole-3-carboxaldehydes and related compounds were synthesized and screened for antitubercular activity against Mycobacterium tuberculosis H37RV in BACTEC 12B medium using the Microplate Alamar Blue Assay (MABA). Several compounds showed inhibitory activity against M. tuberculosis in primary screening assays at a concentration of 6.25 μg/mL; subsequent dose-response studies indicated that the most active compounds, 3d, 3e & 8b, had IC50 values of 5.96, 5.4 & 1.6 μg/mL, respectively. These compounds represent potential leads for the further development of novel antitubercular agents.
ISSN:1475-6366
1475-6374
DOI:10.1080/14756360801915526