Title of article
Discovery of cyclopentane- and cyclohexane-trans-1,3-diamines as potent melanin-concentrating hormone receptor 1 antagonists
Author/Authors
Fabrizio Giordanetto، نويسنده , , Olle Karlsson، نويسنده , , Jan Lindberg، نويسنده , , Lars-Olof Larsson، نويسنده , , Anna Linusson، نويسنده , , Emma Evertsson، نويسنده , , David G.A. Morgan، نويسنده , , Tord Inghardt، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
10
From page
4232
To page
4241
Abstract
We herein report the optimization of cyclopentane- and cyclohexane-1,3-diamine derivatives as novel and potent MCH-R1 antagonists. Structural modifications of the 2-amino-quinoline and thiophene moieties found in the initial lead compound served to improve its metabolic stability profile and MCH-R1 affinity, and revealed unprecedented SAR when compared to other 2-amino-quinoline-containing MCH-R1 antagonists.
Keywords
obesity , Melanin-concentrating hormone receptor , MCH-R1 antagonists , MCH
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798401
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