Structure-activity relationship of (1-aryl-2-piperazinylethyl) piperazines: antagonists for the AGRP/melanocortin receptor binding

PN Arasasingham, C Fotsch, X Ouyang…

Index: Arasasingham, Premilla N.; Fotsch, Christopher; Ouyang, Xiaohu; Norman, Mark H.; Kelly, Michael G.; Stark, Kevin L.; Karbon, Bill; Hale, Clarence; Baumgartner, James W.; Zambrano, Martha; Cheetham, Janet; Tamayo, Nuria A. Journal of Medicinal Chemistry, 2003 , vol. 46, # 1 p. 9 - 11

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Citation Number: 47

Abstract

Agouti-related protein (AGRP) is an endogenous antagonist of the melanocortin action. 1 In the hypothalamus, melanocortin peptide agonists act as satiety-inducing factors that mediate their action through the melanocortin-4 receptor (MC4R) whereas AGRP is an opposing orexigenic agent. Novel inhibitors of the AGRP/MC4 binding based on (piperazinylethyl) piperazines were prepared, and their structure-activity relationship was established.