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Novel HIV-1 protease inhibitors active against multiple PI-resistant viral strains: coadministration with indinavir |
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| Authors: | Kevin Nancy J Duffy Joseph L Kirk Brian A Chapman Kevin T Schleif William A Olsen David B Stahlhut Mark Rutkowski Carrie A Kuo Lawrence C Jin Lixia Lin Jiunn H Emini Emilio A Tata James R |
| Affiliation: | Department of Basic Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. |
| Abstract: | HIV-1 protease inhibitors (PI) with an N-arylpyrrole moiety in the P(3) position afforded excellent antiviral potency and substantially improved aqueous solubility over previously reported variants. The rapid in vitro clearance of these compounds in human liver microsomes prompted oral coadministration with indinavir to hinder their metabolism by the cyctochrome P450 3A4 isozyme and allow for in vivo PK assessment. |
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