Bioorganic & Medicinal Chemistry 2007-06-01

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

Silvia Galiano, Javier Ceras, Nuria Cirauqui, Silvia Pérez, Laura Juanenea, Gildardo Rivera, Ignacio Aldana, Antonio Monge

文献索引：Bioorg. Med. Chem. 15(11) , 3896-911, (2007)

全文：HTML全文

摘要

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).

相关化合物

  • 4-溴苯甲胺

相关文献：

Prokaryotic NavMs channel as a structural and functional model for eukaryotic sodium channel antagonism.

2014-06-10

[Proc. Natl. Acad. Sci. U. S. A. 111(23) , 8428-33, (2014)]

Common metal of copper(0) as an efficient catalyst for preparation of nitriles and imines by controlling additives.

2014-05-30

[Chem. Commun. (Camb.) 50(42) , 5637-40, (2014)]

Postsynthetic modification of peptoids via the Suzuki-Miyaura cross-coupling reaction.

2016-01-01

[Biopolymers 106 , 82-8, (2016)]

Efficient synthesis of 2,6,9-triazabicyclo [3.3.1] nonanes through amine-mediated formal [4+4] reaction of unsaturated imines. Tanaka K, et al.

[Tetrahedron Lett. 53(44) , 5899-5902, (2012)]

Nitrogenous bisabolene sesquiterpenes from marine invertebrates. Gulavita NK, et al.

[J. Org. Chem. 51(26) , 5136-5139, (1986)]

更多文献...