Title of article
Discovery of 1,3-disubstituted-1H-pyrrole derivatives as potent Melanin-Concentrating Hormone Receptor 1 (MCH-R1) antagonists
Author/Authors
Susanne Berglund، نويسنده , , Bryan J. Egner، نويسنده , , Henrik Gradén، نويسنده , , Joakim Gradén، نويسنده , , David G.A. Morgan، نويسنده , , Tord Inghardt، نويسنده , , Fabrizio Giordanetto، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
4859
To page
4863
Abstract
A series of 1,3-disubstituted-1H-pyrrole-based antagonists of the human Melanin-Concentrating Hormone Receptor 1 (h-MCH-R1) are reported. High-throughput screening of the AstraZeneca compound collection yielded 1, a hit with moderate affinity towards MCH-R1. Subsequent structural manipulations and SAR analysis served to rationalize potency requirements, and 12 was identified as a novel, functional MCH-R1 antagonist with favorable pharmacokinetic properties.
Keywords
Melanin-concentrating hormone , MCH-R1 antagonists , obesity , MCH
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799905
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