2. Academic Validation
  3. Design and synthesis of novel, conformationally restricted HMG-CoA reductase inhibitors

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

  • Bioorg Med Chem Lett. 2007 Aug 15;17(16):4531-7. doi: 10.1016/j.bmcl.2007.05.097.
Jeffrey A Pfefferkorn 1,  Chulho Choi,  Yuntao Song,  Bharat K Trivedi,  Scott D Larsen,  Valerie Askew,  Lisa Dillon,  Jeffrey C Hanselman,  Zhiwu Lin,  Gina Lu,  Andrew Robertson,  Catherine Sekerke,  Bruce Auerbach,  Alexander Pavlovsky,  Melissa S Harris,  Graeme Bainbridge,  Nicole Caspers
Affiliations

Affiliation

  • 1 Pfizer Global Research & Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. [email protected]
PMID: 17574411 DOI: 10.1016/j.bmcl.2007.05.097
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.

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