Substituted 5-aroylpyrazine-2-carboxylic acid derivatives: Synthesis and biological activity.
Substituted 5-aroylpyrazine-2-carboxylic acid derivatives: Synthesis and biological activity.
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DOI：
10.1016/s0014-827x(03)00163-0
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发表时间：
2003-11-01
期刊：
影响因子：
--
通讯作者：
Vichova, P.
中科院分区：
文献类型：
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作者：
Dolezal, M.;Jampilek, J.;Vichova, P.
吡嗪环与各种取代芳醛进行均裂芳酰化反应，得到一系列5-芳酰基吡嗪-2-羧酸衍生物。所有化合物的合成方法，分析和光谱数据合成，其初步的体外评价抗结核和抗真菌活性，细胞毒性数据和随后的SAR研究。在制备的所有衍生物中，只有5-（4-氯苯甲酰基）-吡嗪-2-硫代甲酰胺（3d）显示出对结核分枝杆菌的有希望的活性（90%抑制）。最高抗真菌效果（MIC
Homolytic aroylation of pyrazine nucleus with various substituted aromatic carbaldehydes afforded a series of 5-aroylpyrazine-2-carboxylic acid derivatives. The synthetic approach, analytical and spectroscopic data of all compounds synthesized, their preliminary in vitro evaluation of antituberculotic and antifungal activities, cytotoxicity data and subsequent SAR studies are presented. Among all derivatives prepared, only 5-(4-chlorobenzoyl)-pyrazine-2-carbothioamide (3d) showed promising activity (90% inhibition) against Mycobacterium tuberculosis. The highest antifungal effect (MIC