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Bioorg Med Chem Lett. 2003 Aug 4;13(15):2573-6.

The design, synthesis and evaluation of novel HIV-1 protease inhibitors with high potency against PI-resistant viral strains.

Author information

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

Abstract

Replacement of the pyridylmethyl moiety in indinavir with a pyridyl oxazole yielded HIV-1 protease inhibitors (PI) with greatly improved potency against PI-resistant HIV-1 strains. A meta-methoxy group on the pyridyl ring and a gem-dimethyl methyl linkage afforded compound 10 with notable in vitro antiviral activity against HIV-1 viral strains with reduced susceptibility to the clinically available PIs. Compound 10 also demonstrated favorable in vivo pharmacokinetics in animal models.

PMID:
12852969
DOI:
10.1016/s0960-894x(03)00474-8
[Indexed for MEDLINE]

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