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Synthesis and antimycobacterial activity of isoniazid derivatives from renewable fatty acids |
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| Authors: | Marieli O Rodrigues Jéssica B Cantos Caroline R Montes D’Oca Karina L Soares Tatiane S Coelho Luciana A Piovesan Dennis Russowsky Pedro A da Silva Marcelo G Montes D’Oca |
| Institution: | 1. Laboratório Kolbe de Síntese Orgânica, Escola de Química e Alimentos, Universidade Federal do Rio Grande, Rio Grande, RS, Brazil;2. Laboratório de Micobacteriologia, Faculdade de Medicina, Universidade Federal do Rio Grande, Rio Grande, RS, Brazil;3. Laboratório de Síntese Orgânica, Instituto de Química, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil |
| 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. |
| Keywords: | Fatty acids INH-derivatives Antimycobacterial activity |
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