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

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.

Affiliation

Hudson S; Department of Medicinal Chemistry, Neurocrine Biosciences Inc., 12790 El Camino Real, San Diego, CA 92130, USA. shudson@neurocrine.com

Bioorg Med Chem Lett ; 16(18): 4922-30, 2006 Sep 15.

Article de En | MEDLINE | ID: mdl-16824755

ABSTRACT

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.

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Collection: 01-internacional Base de données: MEDLINE Sujet principal: Pyrrolidines / Urée / Récepteur somatostatine Limites: Animals Langue: En Journal: Bioorg Med Chem Lett Sujet du journal: BIOQUIMICA / QUIMICA Année: 2006 Type de document: Article Pays d'affiliation: États-Unis d'Amérique

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