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Title: Synthesis of novel derivatives of 4-amino-3-(2-furyl)-5-mercapto-1,2,4-triazole as potential HIV-1 NNRTIs
Authors: Wu, Jingde ×
Liu, Xinyong
Cheng, Xianchao
Cao, Yuan
Wang, Defeng
Li, Zhong
Xu, Wenfang
Pannecouque, Christophe
Witvrouw, Myriam
De Clercq, Erik #
Issue Date: 9-Oct-2007
Series Title: Molecules (Basel, Switzerland) vol:12 issue:8 pages:2003-2016
Abstract: A series of 5-alkylthio (2a-d), 4-arylideneamino (3a-d) and 4-arylideneamino-5-alkylthio derivatives (4a-f) of 4-amino-3-(2-furyl)-5-mercapto-1,2,4-triazole (1) were synthesized by alkylation of the parent compound with alkyl halides and condensation with aldehydes, respectively. Sulfanyl dimers 5a-d and 4-iminomethyl dimer 6 were correspondingly prepared by reaction with alkane dibromides and 1,4-diformylbenzene. Mannich base 7 was also synthesized by aminomethylation of the 3-sulfanyltriazole 1 at the N1 position. The newly designed and synthesized substituted s-triazole derivatives were assayed for anti-HIV-1 activity by examination of their inhibition of HIV-1-induced cytopathogenicity in MT-4 cells and by determination of their inhibitory effect on HIV-1 reverse transcriptase. Compound 4e was found to be the most active inhibitor against HIV-1 replication in cell culture (EC50 = 12 microM) and against HIV-1 reverse transcriptase (IC50 = 43.5 microM), which provided a good lead for further optimization.
ISSN: 1420-3049
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Molecular Virology and Gene Therapy
Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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