Chemistry, Biological Properties and SAR Analysis of Quinoxalinones

A.      Carta; S.      Piras; G.      Loriga; G.      Paglietti

Abstract

Quinoxaline derivatives have received much attention in recent years owing to their both biological properties and pharmaceutical applications. In this review we focus the attention on quinoxalin-2(3)-ones and quinoxalin-2,3-diones. These derivatives are particularly interesting since some of them showed antimicrobial (against several bacteria, viruses, fungi, etc), or anticancer activities. Furthermore, others are reported to be potent no-NMDA glutamate receptor antagonists, endowed with anxiolytic, deconditioning, analgesic, antispastic, antiallergic, antithrombotic activities. In this article we also report SAR studies and the most important methods of synthesis of the quinoxalin-2(3)-(di)ones.

Keywords: Quinoxalin-2(3)-ones, quinoxalin-2,3-diones, AMPA antagonists, GlyN antagonists, antimicrobial activity, anticancer activity, Pgp antagonists, antiallergic activity, antithrombotic activity, SAR studies