Design, Synthesis and Docking studies of New Quinazolinone Derivatives as Anti-HIV-1 Agents Quinazolinone Derivatives as Anti-HIV-1 Agents
Iranian Journal of Pharmaceutical Sciences,
Vol. 18 No. 1 (2022),
15 January 2022
,
Page 55-64
https://doi.org/10.22037/ijps.v18.41376
Abstract
The Human Immunodeficiency Virus (HIV) infection is a global health challenge that creates an urgent need to develop new therapeutic agents. In this work, a new group of quinazolinone derivatives were designed and synthesized and evaluated their anti-HIV activity. The antiviral assay revealed that some analogues inhibited HIV replication in the cell culture. A docking study using the later crystallographic data available for PFV integrase including its complexes with Mg2+ and dolutegravir, showed that the designed compounds bind into the active site of integrase enzyme such that both carbonyl groups chelate Mg2+ ions. Interestingly, all of the synthesized compounds were found to present no significant cytotoxicity at a concentration of 100 μM. According to the anti-HIV evaluation results, the compound 10f was found as the most active with the inhibition rate of 38%. Therefore, these compounds can provide a very good basis for the development of new anti-HIV agents.
- Anti-HIV-1,
- Design,
- Synthesis,
- Quinazolinone,
- Benzamide,
- Docking studies.
How to Cite
References
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