Discovery and SAR of a series of 4,6-diamino-1,3,5-triazin-2-ol as novel non-nucleoside reverse transcriptase inhibitors of HIV-1.
The discovery and SAR study of a series of 4,6-diamino-1,3,5-triazin-2-ol compounds as novel HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) are reported. The lead compounds in this series showed excellent activity against wild-type and drug-resistant RT enzymes and viral strains. In addition, compounds from this series demonstrated favorable pharmacokinetic profile in rat. A preliminary modeling study was conducted to understand the binding mode of this series of compounds.
Liu
Bin
B
Ansaris, Four Valley Square, 512 E. Township Line Rd, Blue Bell, PA 19422, United States. bliu@ansarisbio.com
Lee
Younghee
Y
Zou
Jinming
J
Petrassi
H Michael
HM
Joseph
Rhoda W
RW
Chao
Wenchun
W
Michelotti
Enrique L
EL
Bukhtiyarova
Marina
M
Springman
Eric B
EB
Dorsey
Bruce D
BD
D000818:Animals; D055808:Drug Discovery; D008958:Models, Molecular; D051381:Rats; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis* / Q000494:pharmacology*
D018894:Reverse Transcriptase Inhibitors; D014227:Triazines