ABSTRACT
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.
Subject(s)
Antitubercular Agents/chemical synthesis , Antitubercular Agents/pharmacology , Fatty Acids/chemistry , Isoniazid/analogs & derivatives , Isoniazid/pharmacology , Mycobacterium tuberculosis/drug effects , Antitubercular Agents/chemistry , Drug Resistance, Bacterial/drug effects , Isoniazid/chemical synthesis , Microbial Sensitivity Tests , Rifampin/pharmacologyABSTRACT
Several quinonoid and phenazine compounds were synthesized in moderate to high yields and showed activity against H(37)Rv, rifampicin and isoniazid-resistance strains of Mycobacterium tuberculosis. The cytotoxity of the compounds were evaluated against human peripheral blood mononuclear cells (PBMC) and these substances emerge as promising antitubercular prototypes.
