一些杂芳基羧氨基腙衍生物的合成及其抑菌活性。

Drug design and discovery Pub Date : 1998-10-01

D C Billington, M D Coleman, J Ibiabuo, P A Lambert, D L Rathbone, K J Tims

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摘要

自动合成了一系列吡啶-2-、吡嗪-2-和喹啉-2-carboxamidrazone衍生物，并进行了对福氏分枝杆菌的快速筛选。进一步研究了7个吡啶-2- carboxamidra酮衍生物，发现其中4个具有抑制活性，其中化合物4af活性最高。讨论了结构活动性的含义。

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Synthesis and antimycobacterial activity of some heteroarylcarboxamidrazone derivatives.

A series of pyridine-2-, pyrazine-2- and quinoline-2-carboxamidrazone derivatives was prepared in an automated fashion and tested against Mycobacterium fortuitum in a rapid screen. Seven pyridine-2-carboxamidrazone derivatives were investigated further and four were found to have inhibitory activity with compound 4af being the most active. The structure activity implications are discussed.

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Drug design and discovery

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