A potent and orally active HIV-1 integrase inhibitor.
A 1,6-naphthyridine inhibitor of HIV-1 integrase has been discovered with excellent inhibitory activity in cells, good pharmacokinetics, and an excellent ability to inhibit virus with mutant enzyme.
Egbertson
Melissa S
MS
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. melissa_egbertson@merck.com
Moritz
H Marie
HM
Melamed
Jeffrey Y
JY
Han
Wei
W
Perlow
Debra S
DS
Kuo
Michelle S
MS
Embrey
Mark
M
Vacca
Joseph P
JP
Zrada
Matthew M
MM
Cortes
Amanda R
AR
Wallace
Audrey
A
Leonard
Yvonne
Y
Hazuda
Daria J
DJ
Miller
Michael D
MD
Felock
Peter J
PJ
Stillmock
Kara A
KA
Witmer
Marc V
MV
Schleif
William
W
Gabryelski
Lori J
LJ
Moyer
Gregory
G
Ellis
Joan D
JD
Jin
Lixia
L
Xu
Wei
W
Braun
Matthew P
MP
Kassahun
Kellem
K
Tsou
Nancy N
NN
Young
Steven D
SD
D000284:Administration, Oral; D000818:Animals; D002478:Cells, Cultured; D019427:HIV Integrase / Q000187:drug effects / Q000235:genetics; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics* / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D009154:Mutation; D009287:Naphthyridines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship
D019428:HIV Integrase Inhibitors; D009287:Naphthyridines; D019427:HIV Integrase