Design and synthesis of highly potent HIV protease inhibitors with activity against resistant virus.
A series of highly potent HIV protease inhibitors have been designed and synthesized. These compounds are active against various clinical viral isolates as well as wild-type virus. The synthesis and biological activity of these HIV protease inhibitors are discussed.
Lu
Zhijian
Z
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. zhijian_lu@merck.com
Raghavan
Subharekha
S
Bohn
Joann
J
Charest
Mark
M
Stahlhut
Mark W
MW
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
D000588:Amines; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002460:Cell Line; D015195:Drug Design; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006571:Heterocyclic Compounds; D006801:Humans; D020128:Inhibitory Concentration 50; D009154:Mutation; D009842:Oligopeptides / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014779:Virus Replication / Q000187:drug effects
D000588:Amines; D019380:Anti-HIV Agents; D017320:HIV Protease Inhibitors; D006571:Heterocyclic Compounds; D009842:Oligopeptides