Antioxidant and ROS Inhibitory Activities of Heterocyclic 2-Aryl-4(3H)-quinazolinone Derivatives

Title:Antioxidant and ROS Inhibitory Activities of Heterocyclic 2-Aryl-4(3H)-quinazolinone Derivatives

Volume: 18 Issue: 8

Author(s): Shahida Perveen*, Syed Muhammad Saad, Khalid Mohammed Khan and Muhammad Iqbal Choudhary

Affiliation:

• H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270,Pakistan

Keywords: 2-Aryl-4(3H)-quinazolinones, superoxide anion radical scavengers, DPPH assay, ROS inhibition, oxidative stress, antioxidant activities.

Abstract:

Background: Antioxidants are small molecules that prevent or delay the process of oxidations caused by highly reactive free radicals. These molecules are known for their ability to protect various cellular architecture and other biomolecules from oxidative stress and free radicals. Thus, antioxidants play a key role in the prevention of oxidative damages caused by highly reactive free radicals.

Methods: In the present study, a series of previously synthesized heterocyclic 2-aryl-4(3H)- quinazolinone derivatives 1-25 were screened for antioxidant activity by employing in vitro DPPH and superoxide anion radical scavenging activities. ROS inhibitory activities were also evaluated by serum-opsonized zymosan activated whole blood phagocytes and isolated neutrophils. Cytotoxicity studies were carried out by employing an MTT assay against the 3T3 cell line.

Results: Most of the 2-aryl-4(3H)-quinazolinone derivatives showed potent antioxidant activities in superoxide anion radical scavenging assay with IC₅₀ value ranging between 0.57 μM - 48.93 μM, as compared to positive control quercetin dihydrate (IC₅₀ = 94.1 ± 1.1 μM ). Compounds 5, 6, and 14 showed excellent activity in DPPH assay. Compounds 5-8, 12-15, 17, and 20 showed promising activities in the ROS inhibition assay. All compounds were found to be non-cytotoxic against the 3T3 cell line. Structure antioxidant activity has been established.

Conclusion: It can be concluded that most of the heterocyclic 2-aryl-4(3H)-quinazolinone derivatives 1-25 are identified as promising antioxidant agents that are capable of fighting against free radicals and oxidative stress. Thus, they can serve as a lead towards treating oxidative stress and related pathologies.

Cite this article as:

Perveen Shahida *, Saad Muhammad Syed , Khan Mohammed Khalid and Choudhary Iqbal Muhammad , Antioxidant and ROS Inhibitory Activities of Heterocyclic 2-Aryl-4(3H)-quinazolinone Derivatives, Letters in Drug Design & Discovery 2021; 18 (8) . https://dx.doi.org/10.2174/1570180818666210427092319