Bioorganic and Medicinal Chemistry Letters p. 999 - 1004 (2005)
Update date:2022-07-29
Topics:
Grey, Jonathan
Dyck, Brian
Rowbottom, Martin W.
Tamiya, Junko
Vickers, Troy D.
Zhang, Mingzhu
Zhao, Liren
Heise, Christopher E.
Schwarz, David
Saunders, John
Goodfellow, Val S.
Ureas derived from two substituted 3-aminopyrrolidine subunits were prepared as constrained analogs of a linear lead compound and tested as antagonists of the MCH1 receptor. The series was optimized for substitution and stereochemistry to generate a functional antagonist with a Ki of 3.3 nM and IC50 of 12 nM (GTPγS).
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