杂环化合物抗利什曼原虫活性的探索；其体内和体外生物评价结果。
Exploration of antileishmanial activity in heterocycles; results of their in vivo & in vitro bioevaluations.
作者信息
Bhatnagar S, Guru P Y, Katiyar J C, Srivastava R, Mukherjee A, Akhtar M S, Seth M, Bhaduri A P
出版信息
Indian J Med Res. 1989 Nov;89:439-44.
A total of 51 imidazoles, pyrroles, quinolines and isoxazolines compounds were screened for antileishmanial activity in vivo and in vitro, using Leishmania donovani as the test parasite. The screening revealed hitherto unknown antileishmanial activity in these heterocycles. Three of the compounds screened (one belonging to isoxazoline series and two from pyrrole series) showed significant anti-leishmanial activity, ranging from 86-91 per cent inhibition in hamsters. When tested in vitro, using macrophage amastigote culture system, these compounds showed inhibition of 62-78 per cent at 30 micrograms/ml concentration.
以杜氏利什曼原虫为测试寄生虫，对总共51种咪唑、吡咯、喹啉和异恶唑啉化合物进行了体内和体外抗利什曼原虫活性筛选。筛选发现这些杂环化合物具有前所未知的抗利什曼原虫活性。所筛选的化合物中有三种（一种属于异恶唑啉系列，两种来自吡咯系列）表现出显著的抗利什曼原虫活性，在仓鼠体内的抑制率为86% - 91%。在体外使用巨噬细胞无鞭毛体培养系统进行测试时，这些化合物在30微克/毫升浓度下的抑制率为62% - 78%。
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