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 H37R(V) 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 microg/mL; subsequent dose-response studies indicated that the most active compounds, 3d, 3e & 8b, had IC(50) values of 5.96, 5.4 & 1.6 microg/mL, respectively. These compounds represent potential leads for the further development of novel antitubercular agents.
Sonar
Vijayakumar N
VN
Department of Pharmaceutical Sciences, College of Pharmacy, Lexington, USA.
Crooks
Peter A
PA
D000447:Aldehydes / Q000737:chemistry; D000995:Antitubercular Agents / Q000138:chemical synthesis*; D004305:Dose-Response Relationship, Drug; D006835:Hydrazones / Q000138:chemical synthesis* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D014753:Vinyl Compounds / Q000138:chemical synthesis* / Q000494:pharmacology
D000447:Aldehydes; D000995:Antitubercular Agents; D006835:Hydrazones; D014753:Vinyl Compounds