Novel series of substituted biphenylmethyl urea derivatives as MCH-R1 antagonists for the treatment of obesity

…, N Cirauqui, S Pérez, L Juanenea, G Rivera…

Index: Galiano, Silvia; Ceras, Javier; Cirauqui, Nuria; Perez, Silvia; Juanenea, Laura; Rivera, Gildardo; Aldana, Ignacio; Monge, Antonio Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 11 p. 3896 - 3911

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Citation Number: 11

Abstract

We have designed and synthesized two novel series of MCH-R1 antagonists based on a substituted biphenylmethyl urea core. SAR was explored, suggesting that optimal binding with the receptor was achieved when the biphenylmethyl group and the linker were substituted on the same nitrogen of the urea moiety. Compound 1-(3′-cyano-4- biphenylmethyl)-3-(2-hydroxy-1, 1-dimethylethyl)-1-{2-[1-(4-methylbenzyl)-4-piperidinyl] ...