| Autor: |
Erik De Clercq, Myriam Witvrouw, Christophe Pannecouque, Wenfang Xu, Zhong Li, Defeng Wang, Yuan Cao, Xianchao Cheng, Xinyong Liu, Jingde Wu |
| Jazyk: |
angličtina |
| Rok vydání: |
2007 |
| Předmět: |
|
| Zdroj: |
Molecules, Vol 12, Iss 8, Pp 2003-2016 (2007) |
| Druh dokumentu: |
article |
| ISSN: |
1420-3049 |
| DOI: |
10.3390/12082003 |
| Popis: |
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 μM) and against HIV-1 reverse transcriptase (IC50 = 43.5 μM), which provided a good lead for further optimization. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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