|
|||||
|
|
Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 2 |
|
| Authors: | Hudson Sarah Kiankarimi Mehrak Rowbottom Martin W Vickers Troy D Wu Dongpei Pontillo Joseph Ching Brett Dwight Wesley Goodfellow Val S Schwarz David Heise Christopher E Madan Ajay Wen Jenny Ban William Wang Hua Wade Warren S |
| Institution: | Department of Medicinal Chemistry, Neurocrine Biosciences Inc., 12790 El Camino Real, San Diego, CA 92130, USA. shudson@neurocrine.com |
| Abstract: | The design, synthesis, and SAR of a series of retro bis-aminopyrrolidine ureas are described. Compounds from this series exhibited considerable binding affinity (Ki = 1 nM) and functional activity at MCH-R1, acceptable CYP2D6 inhibition, and good rat brain exposure. |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |