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Bis(aminopyrrolidine)-derived ureas (APUs) as potent MCH1 receptor antagonists.

Abstract：

:Ureas derived from two substituted 3-aminopyrrolidine subunits were prepared as constrained analogs of a linear lead compound and tested as antagonists of the MCH(1) receptor. The series was optimized for substitution and stereochemistry to generate a functional antagonist with a K(i) of 3.3 nM and IC(50) of 12 nM (GTPgammaS).

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Grey J,Dyck B,Rowbottom MW,Tamiya J,Vickers TD,Zhang M,Zhao L,Heise CE,Schwarz D,Saunders J,Goodfellow VS

doi

10.1016/j.bmcl.2004.12.036

subject

Has Abstract

pub_date

2005-02-15 00:00:00

pages

999-1004

issue

4

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(04)01496-9

journal_volume

15

pub_type

杂志文章

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