| Autor: |
Meyers KM; Procter & Gamble Pharmaceuticals, 8700 Mason-Montgomery Road, Mason, OH 45039, USA., Méndez-Andino JL, Colson AO, Warshakoon NC, Wos JA, Mitchell MC, Hodge KM, Howard JM, Ackley DC, Holbert JK, Mittelstadt SW, Dowty ME, Obringer CM, Reizes O, Hu XE |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Feb 01; Vol. 17 (3), pp. 819-22. Date of Electronic Publication: 2006 Oct 25. |
| DOI: |
10.1016/j.bmcl.2006.10.052 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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