Synthesis and antimycobacterial activity of isoniazid derivatives from renewable fatty acids

被引：46
作者：
Rodrigues, Marieli O. [1 ]
Cantos, Jessica B. [2 ]
Montes D'Oca, Caroline R. [3 ]
Soares, Karina L. [1 ]
Coelho, Tatiane S. [2 ]
Piovesan, Luciana A. [1 ]
Russowsky, Dennis [3 ]
da Silva, Pedro A. [2 ]
Montes D'Oca, Marcelo G. [1 ]
机构：
[1] Univ Fed Rio Grande, Lab Kolbe Sintese Organ, Escola Quim & Alimentos, Rio Grande, RS, Brazil
[2] Univ Fed Rio Grande, Lab Micobacteriol, Fac Med, Rio Grande, RS, Brazil
[3] Univ Fed Rio Grande do Sul, Lab Sintese Organ, Inst Quim, Porto Alegre, RS, Brazil
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2013年 / 21卷 / 22期
关键词：
Fatty acids; Mycobacterium tuberculosis; INH-derivatives; Antimycobacterial activity; MYCOBACTERIUM-TUBERCULOSIS; CONSTITUENTS;
D O I：
10.1016/j.bmc.2013.09.034
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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. (C) 2013 Elsevier Ltd. All rights reserved.
引用
收藏
页码：6910 / 6914
页数：5
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