Novel 3,4-dihydroquinolin-2(1H)-one inhibitors of human glycogen phosphorylase a.

Article Details

Citation

Rosauer KG, Ogawa AK, Willoughby CA, Ellsworth KP, Geissler WM, Myers RW, Deng Q, Chapman KT, Harris G, Moller DE

Novel 3,4-dihydroquinolin-2(1H)-one inhibitors of human glycogen phosphorylase a.

Bioorg Med Chem Lett. 2003 Dec 15;13(24):4385-8.

PubMed ID
14643331 [ View in PubMed
]
Abstract

The preparation of a series of substituted indoles coupled to six- and seven-membered cyclic lactams is described and their role as human glycogen phosphorylase a inhibitors discussed. The SAR of the indole moiety and lactam ring are presented.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
Cp403700, (S)-1-{2-[(5-Chloro-1h-Indole-2-Carbonyl)-Amino]-3-Phenyl-Propionyl}-Azetidine-3-CarboxylateGlycogen phosphorylase, liver formIC 50 (nM)45N/AN/ADetails