Title of article
Aminomethyl tetrahydronaphthalene ketopiperazine MCH-R1 antagonists—Increasing selectivity over hERG
Author/Authors
Kenneth M. Meyers، نويسنده , , Jose L. Mendez-Andino، نويسنده , , Anny-Odile Colson، نويسنده , , Namal C. Warshakoon، نويسنده , , John A. Wos، نويسنده , , Maria C. Mitchell، نويسنده , , Karen M. Hodge، نويسنده , , Jeremy M. Howard، نويسنده , , David C. Ackley، نويسنده , , Jerry K. Holbert، نويسنده , , Scott W. Mittelstadt، نويسنده , , Martin E. Dowty، نويسنده , , Cindy M. Obringer، نويسنده , , Ofer Reizes، نويسنده , , X. Eric Hu، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
4
From page
819
To page
822
Abstract
A direct correlation between hERG binding and QTc prolongation was established for a series of aminomethyl tetrahydronaphthalene ketopiperazine MCH-R1 antagonists. Compounds within this class with greater selectivity over hERG were developed. Compound 4h proved to have the best profile, with MCH-R1 Ki = 16 nm and hERG IC50 = 25 μM.
Keywords
Melanin-concentrating hormone , MCH-R1 antagonists , obesity , HERG , QTc prolongation , Aminomethyl tetrahydronaphthalene ketopiperazines
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797747
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