Synthesis and antimycobacterial activity of isoniazid derivatives from renewable fatty acids.
Rodrigues MO, Cantos JB, D'Oca CR, Soares KL, Coelho TS, Piovesan LA, Russowsky D, da Silva PA, D'Oca MG.
This work describes the synthesis of a series of fatty acid hydrazide derivatives of isoniazid (INH). The compounds were tested against Mycobacterium tuberculosis H37Rv (ATCC 27294) as well as INH-resistant (ATCC 35822 and 1896 HF) and rifampicin-resistant (ATCC 35338) M. tuberculosis strains. The fatty acid derivatives of INH showed high antimycobacterial potency against the studied strains, which is desirable for a pharmaceutical compound, suggesting that the increased lipophilicity of isoniazid plays an important role in its antimycobacterial activity.