Novel series of substituted biphenylmethyl urea derivatives as MCH-R1 antagonists for the treatment of obesity |
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Authors: | Galiano Silvia Ceras Javier Cirauqui Nuria Pérez Silvia Juanenea Laura Rivera Gildardo Aldana Ignacio Monge Antonio |
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Affiliation: | Unidad en Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada, University of Navarra, c/Irunlarrea s/n, 31080 Pamplona, Spain. |
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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]ethyl}urea 2t showed the best antagonist binding activity to the MCH-R1 with a 43 nM K(i). |
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