Synthesis, characterization, and investigation of the anti-inflammatory effect of 2,3-disubstituted quinazoline-4(1H)-one

Bhimrao Ghodge,Ajay Kshirsagar,Vijay Navghare

doi:10.1186/s43088-020-00056-w

Abstract

BackgroundQuinazolin-4(1H)-one nucleus has attracted the attention of medicinal chemists due to their clinical uses. Modification of quinazolinone ring for the development of pharmaceutical and clinical compound for its anti-inflammatory potential.ResultsIn vitro anti-inflammatory activity of the synthesized compounds was performed by using egg albumin protein denaturation assay, while in vivo anti-inflammatory activity was performed by using carrageenan-induced rat paw edema and cotton pellet-induced granuloma pouch model.In the present study, we synthesized a new series of 2,3-disubstituted quinazolin-4(1H)-one derivatives and evaluated their in vivo, in vitro anti-inflammatory effect. Their chemical structures are confirmed by FTIR, 1HNMR, and mass spectrum. Among all the synthesized compounds, G1 and G3 exhibit the significant anti-inflammatory activity by inhibiting release of inflammatory mediators like prostaglandin, histamine, and serotonin. in both in vivo and in vitro models as compared to compound G2.ConclusionThese synthesized compounds showed anti-inflammatory activity by inhibiting prostaglandins and COX enzymes. So, all test compounds may be used for both inflammation as well as inflammation-induced cancer therapy. Future various screening method related with inflammation and inflammation-induced cancer needs to be evaluated pre-clinically and clinically.

Highlights

Quinazolin-4(1H)-one nucleus has attracted the attention of medicinal chemists due to their clinical uses
Many efforts have been focused by researchers on the modification of quinazolinone ring for development of pharmaceutical and clinical compound
Long-term clinical usage of Nonsteroidal anti-inflammatory drugs (NSAIDs) is associated with significant side effects such as gastro-intestinal lesions, Ghodge et al Beni-Suef University Journal of Basic and Applied Sciences

Summary

Introduction

Quinazolin-4(1H)-one nucleus has attracted the attention of medicinal chemists due to their clinical uses. Modification of quinazolinone ring for the development of pharmaceutical and clinical compound for its antiinflammatory potential. Quinazolinone nucleus is an interesting molecule among the most important classes of an aromatic bicyclic compound with two nitrogen atoms in structure [1]. It consists of an aromatic benzo pyrimidine system made up of two fused six-member simple aromatic ring benzene and pyrimidine ring [2]. Many efforts have been focused by researchers on the modification of quinazolinone ring for development of pharmaceutical and clinical compound. The present work is to design novel substituted quinazolin-4-(1H)-one derivative and screened for their anti-inflammatory property

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Conclusion