1007877-58-8Relevant articles and documents
INHIBITORS OF CYTOCHROME P450
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, (2015/11/10)
The present application provides for a compound of Formula I, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.
Structure-activity relationships of diamine inhibitors of cytochrome P450 (CYP) 3A as novel pharmacoenhancers, part I: Core region
Liu, Hongtao,Xu, Lianhong,Hui, Hon,Vivian, Randy,Callebaut, Christian,Murray, Bernard P.,Hong, Allen,Lee, Melody S.,Tsai, Luong K.,Chau, Jennifer K.,Stray, Kirsten M.,Cannizzaro, Carina,Choi, You-Chul,Rhodes, Gerry R.,Desai, Manoj C.
, p. 989 - 994 (2014/02/14)
Ritonavir (RTV), an HIV-1 protease inhibitor (PI), is also a potent mechanism-based inhibitor of human cytochrome P450 3A (CYP3A) and has been widely prescribed as a pharmacoenhancer. As a boosting agent for marketed PIs, it reduces pill burden, and improves compliance. Removal of the hydroxyl group from RTV reduces, but does not eliminate HIV PI activity and does not affect CYP3A inhibition. Herein we report the discovery of a novel series of CYP3A inhibitors that are devoid of antiviral activity. The synthesis and evaluation of analogs with extensive modifications of the 1,4-diamine core along with the structure activity relationships with respect to anti-HIV activity, CYP3A inhibitory activity, selectivity against other CYP enzymes and the human pregnane X receptor (PXR) will be discussed.
COMPOSITIONS AND METHODS FOR INHIBITING CYTOCHROME P450
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Page/Page column 46, (2008/06/13)
Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters
