Chemistry, Biological Properties and SAR Analysis of Quinoxalinones

Authors: Carta, A.1; Piras, S.1; Loriga, G.1; Paglietti, G.1

Source: Mini Reviews in Medicinal Chemistry, Volume 6, Number 11, November 2006 , pp. 1179-1200(22)

Publisher: Bentham Science Publishers

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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

Document Type: Research article

DOI: 10.2174/138955706778742713

Affiliations: 1: Dipartimento Farmaco Chimico Tossicologico, Facolta di Farmacia, Universita di Sassari, via Muroni 23/a, 07100 Sassari, Italy.

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