Structure–activity relationship studies on a series of piperazinebenzylalcohols and their ketone and amine analogs as melanocortin-4 receptor ligands

…, FC Tucci, JA Tran, BA Fleck, J Wen, C Chen

文献索引：Marinkovic, Dragan; Tucci, Fabio C.; Tran, Joe A.; Fleck, Beth A.; Wen, Jenny; Chen, Chen Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 17 p. 4817 - 4822

全文：HTML全文

被引用次数: 0

摘要

A series of piperazinebenzylalcohols were prepared and studied to compare with their ketone and amine analogs as MC4R antagonists. Several benzylalcohols such as 14a and 14g displayed low nanomolar binding affinities (Ki< 10nM), and high selectivities over other melanocortin receptor subtypes.