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N-取代的4-重氮基吡唑-5-甲酰胺的合成、抗菌活性及构效关系。2.

Synthesis, antibacterial activity and structure-activity relationships of N-substituted 4-diazo-pyrazole-5-carboxamides. 2.

作者信息

Baraldi P G, Cacciari B, Leoni A, Recanatini M, Roberti M, Rossi M, Manfredini S, Periotto V, Simoni D

机构信息

Dipartimento di Scienze Farmaceutiche, Universitá di Bologna.

出版信息

Farmaco. 1991 Nov;46(11):1337-50.

PMID:1811619
Abstract

A series of 4-diazopyrazole-5-carboxamides 1 d-n has been synthesized and their antibacterial activity against a number of Gram-negative and Gram-positive strains has been tested. Some of the compounds resulted quite active and the whole set allowed to further study the SAR of the class. Substituents in position 5 affect Gram-negative and Gram-positive activities via bulk and electronic properties respectively; position 3 mostly affects the Gram-negative activity, while the presence of the charged diazo group in position 4 is crucial for both antibacterial activities.

摘要

已经合成了一系列4-重氮基吡唑-5-甲酰胺1 d-n,并测试了它们对多种革兰氏阴性和革兰氏阳性菌株的抗菌活性。其中一些化合物表现出相当高的活性,并且整个系列有助于进一步研究该类化合物的构效关系。5位上的取代基分别通过空间位阻和电子性质影响革兰氏阴性和革兰氏阳性活性;3位主要影响革兰氏阴性活性,而4位带电荷的重氮基团的存在对两种抗菌活性都至关重要。

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