Synthesis of novel HIV protease inhibitors (PI) with activity against PI-resistant virus.
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.
Raghavan
Subharekha
S
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. subha_raghavan@merck.com
Lu
Zhijian
Z
Beeson
Teresa
T
Chapman
Kevin T
KT
Schleif
William A
WA
Olsen
David B
DB
Stahlhut
Mark
M
Rutkowski
Carrie A
CA
Gabryelski
Lori
L
Emini
Emilio
E
Tata
James R
JR
D002460:Cell Line; D024882:Drug Resistance, Viral; D015658:HIV Infections / Q000188:drug therapy / Q000821:virology; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D007202:Indicators and Reagents; D019469:Indinavir / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship
D017320:HIV Protease Inhibitors; D007202:Indicators and Reagents; D019469:Indinavir