作为黑皮质素-4受体配体的3-芳基吡咯烷-2-甲酰胺衍生物的设计与合成
Design and synthesis of 3-arylpyrrolidine-2-carboxamide derivatives as melanocortin-4 receptor ligands.
作者信息
Tran Joe A, Tucci Fabio C, Arellano Melissa, Jiang Wanlong, Chen Caroline W, Marinkovic Dragan, Fleck Beth A, Wen Jenny, Foster Alan C, Chen Chen
机构信息
Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.
出版信息
Bioorg Med Chem Lett. 2008 Mar 15;18(6):1931-8. doi: 10.1016/j.bmcl.2008.01.125. Epub 2008 Feb 7.
PMID:18294847
Abstract
Based on 3-phenylpropionamides, a series of 3-arylpyrrolidine-2-carboxamide derivatives was designed and synthesized to study the effect of cyclizations as melanocortin-4 receptor ligands. It was found that the 2R,3R-pyrrolidine isomer possessed the most potent affinity among the four stereoisomers.
摘要
基于3-苯基丙酰胺，设计并合成了一系列3-芳基吡咯烷-2-甲酰胺衍生物，以研究环化作为黑皮质素-4受体配体的作用。结果发现，在四种立体异构体中，2R,3R-吡咯烷异构体具有最强的亲和力。
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