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吡嗪衍生物的研究。第十部分。某些6-环氨基-、6-咪唑基-和三唑基吡嗪-2-羧酸衍生物的合成及其抑菌活性。

Studies on pyrazine derivatives. Part X. Synthesis and tuberculostatic activity of some 6-cyclamino-, 6-imidazolyl--and triazolylpyrazine-2-carboxylic acids derivatives.

作者信息

Foks H, Janowiec M, Pilarski B

出版信息

Pol J Pharmacol Pharm. 1978 Jan-Feb;30(1):105-11.

PMID:77010
Abstract

The 6(2'-methylpiperidine-, 2',6'-dimethylmorpholino-, imidazolyl- and triazolyl)-2-cyanopyrazines were prepared from 2-cyano-6-chloropyrazine. The -CN group was then transformed into COOH, CONH2, CSNH2, CONHNH2, CONHOH and C(NOH)NH2 functions. All compounds obtained were of weak tuberculostatic activity. Comp. 13 was active against isoniazide, capreomycin and ethionamide resistent strains at the concentration range of 31.2--62.5 microgram/cm3.

摘要

6-(2'-甲基哌啶基、2',6'-二甲基吗啉基、咪唑基和三唑基)-2-氰基吡嗪由2-氰基-6-氯吡嗪制备而成。然后将-CN基团转化为COOH、CONH2、CSNH2、CONHNH2、CONHOH和C(NOH)NH2官能团。所得到的所有化合物均具有微弱的抗结核活性。化合物13在31.2 - 62.5微克/立方厘米的浓度范围内对异烟肼、卷曲霉素和乙硫异烟胺耐药菌株具有活性。

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