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Novel HIV-1 protease inhibitors active against multiple PI-resistant viral strains: coadministration with indinavir.

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Kevin NJ,Duffy JL,Kirk BA,Chapman KT,Schleif WA,Olsen DB,Stahlhut M,Rutkowski CA,Kuo LC,Jin L,Lin JH,Emini EA,Tata JR

doi

10.1016/j.bmcl.2003.08.049

subject

Has Abstract

pub_date

2003-11-17 00:00:00

pages

4027-30

issue

22

eissn

0960-894X

issn

1464-3405

pii

S0960894X03009120

journal_volume

13

pub_type

杂志文章

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