Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase.
A new series of 1,2,4-triazoles was synthesized and tested against several NNRTI-resistant HIV-1 isolates. Several of these compounds exhibited potent antiviral activities against efavirenz- and nevirapine-resistant viruses, containing K103N and/or Y181C mutations or Y188L mutation. Triazoles were first synthesized from commercially available substituted phenylthiosemicarbazides, then from isothiocyanates, and later by condensing the desired substituted anilines with thiosemicarbazones.
De La Rosa
Martha
M
Valeant Research & Development, Costa Mesa, CA 92626, USA.
Kim
Hong Woo
HW
Gunic
Esmir
E
Jenket
Cheryl
C
Boyle
Uyen
U
Koh
Yung-Hyo
YH
Korboukh
Ilia
I
Allan
Matthew
M
Zhang
Weijian
W
Chen
Huanming
H
Xu
Wen
W
Nilar
Shahul
S
Yao
Nanhua
N
Hamatake
Robert
R
Lang
Stanley A
SA
Hong
Zhi
Z
Zhang
Zhijun
Z
Girardet
Jean-Luc
JL
D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015497:HIV-1 / Q000187:drug effects / Q000201:enzymology; D015394:Molecular Structure; D009705:Nucleosides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
D004791:Enzyme Inhibitors; D009705:Nucleosides; D014230:Triazoles; D054303:HIV Reverse Transcriptase