Background: Low molecular weight 1-Aryl-1H-1,2,3-triazoles are endowed with various
types of biological activities, such as against cancer, HIV and bacteria. Despite the existence of six different
classes of antiretroviral drugs in clinical use, HIV/AIDS continue to be an on growing public
Objective: In the present study, we synthesized and evaluated thirty 1-Aryl-1H-1,2,3-triazoles against
Method: The compounds were prepared by Huisgen 1,3-dipolar cycloaddition protocol catalyzed by
Cu(I) between aryl azides and propargylic alcohol followed by further esterification and etherification
from a nucleophilic substitution with acid chlorides or alkyl bromides in good yields. The compounds
were submitted to the inhibition of HIV replication and evaluation of their cytotoxicity. Initially, the
compounds were screened at 10 µM and the most active were further evaluated in order to obtain some
Results: Thirty molecules were evaluated, six were selected – because they inhibited more than 80%
HIV replication. We further showed that two of these compounds are 8-times more potent, and less cytotoxic,
than nevirapine, an antiretroviral drug in clinical use.
Conclusion: We identified very simple triazoles with promissing antiretroviral activities that led to the
development of new drugs against AIDS.