Design and synthesis of novel, conformationally restricted HMG-CoA reductase inhibitors.

Article Details

Citation

Pfefferkorn JA, Choi C, Song Y, Trivedi BK, Larsen SD, Askew V, Dillon L, Hanselman JC, Lin Z, Lu G, Robertson A, Sekerke C, Auerbach B, Pavlovsky A, Harris MS, Bainbridge G, Caspers N

Design and synthesis of novel, conformationally restricted HMG-CoA reductase inhibitors.

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4531-7. Epub 2007 Jun 6.

PubMed ID
17574411 [ View in PubMed
]
Abstract

Using structure-based design, a novel series of conformationally restricted, pyrrole-based inhibitors of HMG-CoA reductase were discovered. Leading analogs demonstrated potent inhibition of cholesterol synthesis in both in vitro and in vivo models and may be useful for the treatment of hypercholesterolemia and related lipid disorders.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
Simvastatin3-hydroxy-3-methylglutaryl-coenzyme A reductaseIC 50 (nM)49N/AN/ADetails