Document Type : Research Paper
Authors
1
Department of Pharmaceutical Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran
2
Department of Pharmaceutical Chemistry, Faculty of Pharmaceutical Chemistry, Tehran Medical Sciences, Islamic Azad University, Tehran, Iran
3
Active Pharmaceutical Ingredients Research Center (APIRC), Tehran Medical Sciences, Islamic Azad University, Tehran, Iran
4
1. Pharmaceutical Sciences Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran. 2. Department of Pharmaceutical Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran
5
Medical Lab Technology Department, School of Allied Medical Sciences, Shahid Beheshti University of Medical Sciences, Tehran, Iran
10.22034/ijps.2022.555596.2017
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 antiHIV 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.
Keywords
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