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Design and synthesis of novel, conformationally restricted HMG-CoA reductase inhibitors |
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| Authors: | Pfefferkorn Jeffrey A Choi Chulho Song Yuntao Trivedi Bharat K Larsen Scott D Askew Valerie Dillon Lisa Hanselman Jeffrey C Lin Zhiwu Lu Gina Robertson Andrew Sekerke Catherine Auerbach Bruce Pavlovsky Alexander Harris Melissa S Bainbridge Graeme Caspers Nicole |
| Affiliation: | Pfizer Global Research & Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. jeffrey.a.pfefferkorn@pfizer.com |
| 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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