[具有化疗效果的硝基化合物。第三次通讯：硝基吡啶、硝基咪唑并吡啶及相关化合物（作者译）]

[Chemotherapeutically effective nitro compounds. 3rd communication: nitropyridines, nitroimidazopyridines and related compounds (author's transl)].

作者信息

Winkelmann E, Raether W, Hartung H, Wagner W H

出版信息

Arzneimittelforschung. 1977;27(1):82-9.

Abstract

New 2-nitropyridines and 3-nitropyridines, and 3-nitroimidazo-[1,2-a]-pyridines and related compounds (together 106) were synthesized and tested for their chemotherapeutic efficacy against trichomonads, amoebas and other organisms, such as Eimeria tenella, bacteria, fungi, helminths. Several 2-nitropyridines revelaed a detectable systemic effect against Entamoeba histolytica (extraintestinal amoebiasis of the golden hamster) and also a weak activity against Trichomonas fetus in the NMRI-mouse. Only a few 3-nitropyridines showed a marked systemic effect against trichomonads. Of the 3-nitroimidazo-[1,2-a]-pyridines, only the electroneutral carboxylic acid amide group exhibited a pronounced activity, exclusively against trichomonads; however, the activity was nullified again by electronegative, electropositive and other electroneutral substituents. As they were not superior in chemotherapeutic respect compared to the known standard preparation (metronidazole), no further tests were carried out with the most effective compounds.

摘要

合成了新型2-硝基吡啶和3-硝基吡啶，以及3-硝基咪唑并[1,2-a]吡啶及其相关化合物（共106种），并测试了它们对滴虫、阿米巴原虫以及其他生物体（如柔嫩艾美耳球虫、细菌、真菌、蠕虫）的化疗效果。几种2-硝基吡啶对溶组织内阿米巴（金黄仓鼠的肠外阿米巴病）显示出可检测到的全身作用，并且对NMRI小鼠体内的胎儿三毛滴虫也有微弱活性。只有少数3-硝基吡啶对滴虫显示出明显的全身作用。在3-硝基咪唑并[1,2-a]吡啶中，只有电中性的羧酸酰胺基团表现出显著活性，且仅针对滴虫；然而，电负性、电正性和其他电中性取代基会再次使其活性丧失。由于与已知标准制剂（甲硝唑）相比，它们在化疗方面并不优越，因此未对最有效的化合物进行进一步测试。