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

Index: 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

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Abstract

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.