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Bioorg Med Chem Lett. 2002 Feb 25;12(4):529-32.

A combinatorial library of indinavir analogues and its in vitro and in vivo studies.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. yuan_cheng@merck.com

Abstract

A combinatorial library of 300HIV protease inhibitors has been synthesized. The library was screened against recombinant wild-type and mutant HIV-1 protease enzymes. The pharmacokinetics of the library was evaluated by dosing in dogs. Compounds that are notably more potent than indinavir and have favorable pharmacokinetic properties were identified.

PMID:
11844665
DOI:
10.1016/s0960-894x(01)00824-1
[Indexed for MEDLINE]

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