Synthesis and structure–activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone …

…, B Ching, W Dwight, VS Goodfellow, D Schwarz…

Index: 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. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 18 p. 4922 - 4930

Full Text: HTML

Citation Number: 10

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= 1nM) and functional activity at MCH-R1, acceptable CYP2D6 inhibition, and good rat brain exposure.