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某些N-取代2-氯吲哚-3-甲醛的N-甲基硝酮和硝基乙烯基衍生物的合成及其体外抗菌活性

[Synthesis and in vitro antibacterial activity of N-methylnitrone and nitrovinyl derivatives of some N-substituted 2-chloroindol-3-carboxaldehydes].

作者信息

Gatti R, Cavrini V, Roveri P, Bianucci F, Legnani P

出版信息

Farmaco Sci. 1981 Feb;36(2):102-8.

PMID:7227499
Abstract

N-methylnitrones and nitrovinyl derivatives from 1-substituted-2-chloroindol-3-carboxaldehydes were synthesized and evaluated for their in vitro antibacterial activity. Some nitrovinyl derivatives displayed good in vitro activity against Gram-positive bacteria; the compound (II e), 1-(o-chlorobenzyl)-2-chloro-3-(2-nitroethenyl)indole, was more active than nitrofurantoin against Staphylococcus aureus and Streptococcus pyogenes. Some structure-activity relationships are discussed.

摘要

合成了1-取代-2-氯吲哚-3-甲醛的N-甲基硝酮和硝基乙烯基衍生物,并对其体外抗菌活性进行了评估。一些硝基乙烯基衍生物对革兰氏阳性菌显示出良好的体外活性;化合物(II e),1-(邻氯苄基)-2-氯-3-(2-硝基乙烯基)吲哚,对金黄色葡萄球菌和化脓性链球菌的活性比呋喃妥因更强。讨论了一些构效关系。

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