Structure–activity relationships of trans-substituted-propenoic acid derivatives on the nicotinic acid receptor HCA2 (GPR109A)

…, CC Blad, CM Artsen, C Klopman, DR Wolfram…

Index: Van Veldhoven; Blad; Artsen; Klopman; Wolfram; Abdelkadir; Lane; Brussee; Ijzerman Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 9 p. 2736 - 2739

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Citation Number: 7

Abstract

Nicotinic acid (niacin) has been used for decades as an antidyslipidemic drug in man. Its main target is the hydroxy-carboxylic acid receptor HCA2 (GPR109A), a G protein-coupled receptor. Other acids and esters such as methyl fumarate also interact with the receptor, which constituted the basis for the current study. We synthesized a novel series of substituted propenoic acids, such as fumaric acid esters, fumaric acid amides and ...