488097-05-8Relevant academic research and scientific papers
Synthesis and anti-HIV evaluation of novel 1,2,4-triazole derivatives as potential non-nucleoside HIV-1 reverse transcriptase inhibitors
Li, Zhenyu,Cao, Yuan,Zhan, Peng,Pannecouque, Christophe,Balzarini, Jan,De Clercq, Erik,Liu, Xinyong
, p. 27 - 34 (2013/08/22)
A series of novel 1,2,4-triazole derivatives has been designed and synthesized. All of the new compounds were evaluated for their anti-HIV activities in MT-4 cells. Three of them showed moderate activities against wild-type HIV-1 with an EC50 r
Synthesis of novel derivatives of 4-amino-3-(2-furyl)-5-mercapto-1,2,4- triazole as potential HIV-1 NNRTIs
Wu, Jingde,Liu, Xinyong,Cheng, Xianchao,Cao, Yuan,Wang, Defeng,Li, Zhong,Xu, Wenfang,Pannecouque, Christophe,Witvrouw, Myriam,De Clercq, Erik
, p. 2003 - 2016 (2008/02/08)
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 N 1 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 μM) and against HIV-1 reverse transcriptase (IC 50 = 43.5 μM), which provided a good lead for further optimization.
