College of Pharmacy, University of Hawai'i at Hilo, Hilo, HI 96720-4029 (USA); Interdepartmental Center Biopharmanet_TEC, Universita' degli Studi di Parma, Via G. P. Usberti 27, Parma (Italy).
ChemMedChem. 2012 Nov;7(11):1895-900. doi: 10.1002/cmdc.201200346. Epub 2012 Sep 17.
Clear and rational thinking: A series of rationally designed, lansine-derived carbazoles was synthesized and evaluated for activity against promastigotes and amastigotes of Leishmania donovani, the causative agent of leishmaniasis. Some structural modifications gave rise to compounds with enhanced activity and selectivity over lansine, allowing structure-activity relationships to be elucidated and providing a foundation for the further development of this pharmacophore.
我们设计并合成了一系列结构合理的源于 Lansine 的咔唑类化合物，评估其对引起利什曼病的利什曼原虫的前鞭毛体和无鞭毛体的活性。一些结构修饰使化合物的活性和选择性相对于 Lansine 增强，使我们能够阐明构效关系，并为进一步开发这一药效团提供了基础。
