Orally bioavailable highly potent HIV protease inhibitors against PI-resistant virus.
Efforts directed to identifying potent HIV protease inhibitors (PI) have yielded a class of compounds that are not only very active against wild-type (NL4-3) HIV virus but also very potent against a panel of PI-resistant viral isolates. Chemistry and biology are described.
Lu
Zhijian
Z
Department of Basic Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. Zhijian_lu@merck.com
Bohn
Joann
J
Rano
Tom
T
Rutkowski
Carrie A
CA
Simcoe
Amy L
AL
Olsen
David B
DB
Schleif
William A
WA
Carella
Anthony
A
Gabryelski
Lori
L
Jin
Lixia
L
Lin
Jiunn H
JH
Emini
Emilio
E
Chapman
Kevin
K
Tata
James R
JR
D000284:Administration, Oral; D001682:Biological Availability; D024882:Drug Resistance, Viral; D006678:HIV / Q000187:drug effects* / Q000201:enzymology; D016333:HIV Protease / Q000187:drug effects; D017320:HIV Protease Inhibitors / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology*; D019469:Indinavir / Q000031:analogs & derivatives*; D015394:Molecular Structure
D017320:HIV Protease Inhibitors; D019469:Indinavir; D016333:HIV Protease