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Bioorg Med Chem Lett. 2007 Feb 1;17(3):819-22. Epub 2006 Oct 25.

Aminomethyl tetrahydronaphthalene ketopiperazine MCH-R1 antagonists--Increasing selectivity over hERG.

Author information

1
Procter & Gamble Pharmaceuticals, 8700 Mason-Montgomery Road, Mason, OH 45039, USA.

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 microM.

PMID:
17107796
DOI:
10.1016/j.bmcl.2006.10.052
[Indexed for MEDLINE]

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