New Heterocyclic Hydrazones in the Search for Antitubercular Agents: Synthesis and In Vitro Evaluations
Sixteen pyrrole containing hydrazones were synthesized from isoniazid (INH) or from 1H-1- pyrrolylcarbohydrazides. Nine products exhibited 92-100% inhibitory activity against Mycobacterium tuberculosis H37Rv at 6.25 μg/mL (Microplate Alamar Blue Assay). Two leads showed MICs 0.78 and > 0.1 μg/mL, SIs > 12.82 and > 100. "Drug likeness" was assessed by "Lipinski rule of five".
Keywords: Carbohydrazides, Hydrazones, Pyrrole, Synthesis, Tuberculostatics
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