title: Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase.
abstract: 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.
authors.affiliation: Valeant Research & Development, Costa Mesa, CA 92626, USA.
authors.forename: Martha
authors.initials: M
authors.lastname: De La Rosa
authors.forename: Hong Woo
authors.initials: HW
authors.lastname: Kim
authors.forename: Esmir
authors.initials: E
authors.lastname: Gunic
authors.forename: Cheryl
authors.initials: C
authors.lastname: Jenket
authors.forename: Uyen
authors.initials: U
authors.lastname: Boyle
authors.forename: Yung-Hyo
authors.initials: YH
authors.lastname: Koh
authors.forename: Ilia
authors.initials: I
authors.lastname: Korboukh
authors.forename: Matthew
authors.initials: M
authors.lastname: Allan
authors.forename: Weijian
authors.initials: W
authors.lastname: Zhang
authors.forename: Huanming
authors.initials: H
authors.lastname: Chen
authors.forename: Wen
authors.initials: W
authors.lastname: Xu
authors.forename: Shahul
authors.initials: S
authors.lastname: Nilar
authors.forename: Nanhua
authors.initials: N
authors.lastname: Yao
authors.forename: Robert
authors.initials: R
authors.lastname: Hamatake
authors.forename: Stanley A
authors.initials: SA
authors.lastname: Lang
authors.forename: Zhi
authors.initials: Z
authors.lastname: Hong
authors.forename: Zhijun
authors.initials: Z
authors.lastname: Zhang
authors.forename: Jean-Luc
authors.initials: JL
authors.lastname: Girardet
mesh_terms: 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*
chemical_list: D004791:Enzyme Inhibitors; D009705:Nucleosides; D014230:Triazoles; D054303:HIV Reverse Transcriptase