Design and synthesis of novel, conformationally restricted HMG-CoA reductase inhibitors.
Article Details
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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
Drug Target Property Measurement pH Temperature (°C) Simvastatin 3-hydroxy-3-methylglutaryl-coenzyme A reductase IC 50 (nM) 49 N/A N/A Details