Synthesis and evaluation of inhibitors of cytochrome P450 3A (CYP3A) for pharmacokinetic enhancement of drugs

CA Flentge, JT Randolph, PP Huang, LL Klein…

Index: Flentge, Charles A.; Randolph, John T.; Huang, Peggy P.; Klein, Larry L.; Marsh, Kennan C.; Harlan, John E.; Kempf, Dale J. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 18 p. 5444 - 5448

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Citation Number: 8

Abstract

The HIV protease inhibitor ritonavir (RTV) is also a potent inhibitor of the metabolizing enzyme cytochrome P450 3A (CYP3A) and is clinically useful in HIV therapy in its ability to enhance human plasma levels of other HIV protease inhibitors (PIs). A novel series of CYP3A inhibitors was designed around the structural elements of RTV believed to be important to CYP3A inhibition, with general design features being the attachment of ...