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海洋生物碱的合成:8,9-二氢科斯西酰胺B及其类似物作为新型抗利什曼原虫剂

Synthesis of marine alkaloid: 8,9-dihydrocoscinamide B and its analogues as Novel class of antileishmanial agents.

作者信息

Gupta Leena, Talwar Archna, Palne Shraddha, Gupta Suman, Chauhan Prem M S

机构信息

Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226001, India.

出版信息

Bioorg Med Chem Lett. 2007 Jul 15;17(14):4075-9. doi: 10.1016/j.bmcl.2007.04.035. Epub 2007 Apr 19.

Abstract

A series of marine alkaloid 8,9-dihydrocoscinamide B, its analogues and indolylglyoxylamide derivatives have been synthesized and screened for their in vitro antileishmanial activity profile in promastigote and amastigote models. Compounds 7 and 10 have shown 99-100% inhibition against promastigotes and 97-98% inhibition against amastigotes at a concentration of 10 microg/ml.

摘要

已经合成了一系列海洋生物碱8,9-二氢科斯西酰胺B、其类似物和吲哚基乙二醛酰胺衍生物,并在前鞭毛体和无鞭毛体模型中对它们的体外抗利什曼原虫活性进行了筛选。化合物7和10在浓度为10微克/毫升时,对前鞭毛体的抑制率为99 - 100%,对无鞭毛体的抑制率为97 - 98%。

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