Abstract
BackgroundThree lipophilic isoniazid (INH) derivatives, 1-isonicotinoyl-2-hexadecanoyl hydrazine (INH-C16), 1-isonicotinoyl-2-heptadecanoyl hydrazine (INH-C17) and 1-isonicotinoyl-2-octadecanoyl hydrazine (INH-C18) were chemically synthesized by attaching the INH to a 16, 17 and an 18-carbon hydrophobic moiety respectively. This paper reports the anti-TB activity of these derivatives and their interactions with INH, streptomycin (STR), rifampicin (RIF), and ethambutol (EMB). MethodsThe anti-TB activity of these derivatives and the first-line drugs was carried out by determining the minimum inhibitory concentration (MIC) against Mycobacterium tuberculosis H37Rv and clinical isolates using tetrazolium microplate assay (TEMA). The interaction study was performed using fixed-ratio method based on TEMA on M. tuberculosis H37Rv. Results and discussionINH-C16, INH-C17 and INH-C18 were displayed good anti-TB activity against the strains tested. In combination, INH-C16 and INH-C18 showed additive/indifferent interaction with INH and EMB, and synergistic interaction with STR and RIF. INH-C17 showed synergism with RIF and additive/indifferent interaction with INH, STR and EMB. ConclusionINH-C16, INH-C17 and INH-C18 have the potential to be drugs lead worthy of further investigations.
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