Background:
Although major efforts have been devoted to the effective treatment of
HIV-1 infection, it has remained one of the leading causes of deaths around the world. So, development
of anti-HIV-1 agents featuring novel structure is essential.
Objective:
To synthesize novel quinazolinone derivatives and evaluate their anti-HIV-1 activity.
Method:
In this study, we designed and synthesized a series of novel 2,3-diaryl-4-quinazolinone derivatives
using a one-pot multicomponent reaction. Then, the resulting derivatives were evaluated
for anti-HIV-1 activity using Hela cell-based single-cycle replication assay.
Results:
Most of the compounds showed efficacy against HIV-1 replication and the compound 9c
exhibited the highest activity with EC50 value of 37 μM. Docking studies indicated that synthesized
compounds can interact with the key residues of the HIV-1 integrase active site. Binding of the most
active compound was consistent with the HIV-1 integrase inhibitors.
Conclusion:
Based on our results, these derivatives represent novel lead compounds for the development
of new promising anti-HIV-1 agents.
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