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寻找抗克氏锥虫药物:来自小鼠模型的新线索。

In search of anti-Trypanosoma cruzi drugs: new leads from a mouse model.

作者信息

Kinnamon K E, Steck E A, Hanson W L, Chapman W L

出版信息

J Med Chem. 1977 Jun;20(6):741-4. doi: 10.1021/jm00216a001.

Abstract

Nine of 25 carefully selected compounds (from a stock of more than 200 000 chemical species amassed principally as a result of testing against other parasitic diseases) were found to have significant suppressive activity against the parasites in the blood of a Trypanosoma cruzi mouse model. Eight of these compounds evaluated in this model had suppressive activity equal to or greater than the reference compound, nifurtimox. For the first time, suppressive activity against T. cruzi is reported for a 7-aminoquinoline, a phosphonium salt, and TAC pamoate; The biological model is believed to be able to serve as a means of identifying other new "leads* in seeking drugs broadly effective against T=ruzi infections in man.

摘要

在25种精心挑选的化合物(主要从超过20万种化学物质的储备中选出,这些储备主要是由于针对其他寄生虫病进行测试而积累的)中,发现有9种对克氏锥虫小鼠模型血液中的寄生虫具有显著的抑制活性。在该模型中评估的这些化合物中有8种的抑制活性等于或大于参考化合物硝呋替莫。首次报道了7-氨基喹啉、一种鏻盐和扑酸苄酚宁对克氏锥虫的抑制活性;该生物学模型被认为能够作为一种手段,在寻找对人类克氏锥虫感染具有广泛疗效的药物时识别其他新的“先导化合物”。

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