Synthesis of novel HIV protease inhibitors (PI) with activity against PI-resistant virus

Subharekha Raghavan; Zhijian Lu; Teresa Beeson; Kevin T Chapman; William A Schleif; David B Olsen; Mark Stahlhut; Carrie A Rutkowski; Lori Gabryelski; Emilio Emini; James R Tata

doi:10.1016/j.bmcl.2007.07.040

Synthesis of novel HIV protease inhibitors (PI) with activity against PI-resistant virus

Bioorg Med Chem Lett. 2007 Oct 1;17(19):5432-6. doi: 10.1016/j.bmcl.2007.07.040. Epub 2007 Jul 31.

Authors

Subharekha Raghavan¹, Zhijian Lu, Teresa Beeson, Kevin T Chapman, William A Schleif, David B Olsen, Mark Stahlhut, Carrie A Rutkowski, Lori Gabryelski, Emilio Emini, James R Tata

Affiliation

¹ Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. [email protected]

PMID: 17692518
DOI: 10.1016/j.bmcl.2007.07.040

Abstract

A series of HIV protease inhibitors with modifications on the P3 position have been designed and synthesized. These compounds exhibit excellent antiviral activity against both the wild type enzyme and PI-resistant clinical viral isolates. The synthesis and biological activity of the compounds are described.

MeSH terms

Cell Line
Drug Resistance, Viral
HIV Infections / drug therapy
HIV Infections / virology
HIV Protease Inhibitors / chemical synthesis*
HIV Protease Inhibitors / pharmacology*
HIV-1 / drug effects*
Humans
Indicators and Reagents
Indinavir / chemical synthesis
Indinavir / pharmacology
Structure-Activity Relationship

Substances

HIV Protease Inhibitors
Indicators and Reagents
Indinavir