917354-59-7Relevant articles and documents
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
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.
, p. 4922 - 4930 (2007/10/03)
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.