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Bioorg Med Chem Lett. 2003 Nov 17;13(22):4027-30.

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

Author information

1
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.

PMID:
14592500
DOI:
10.1016/j.bmcl.2003.08.049
[Indexed for MEDLINE]

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