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Quinoxaline 1,4-Dioxide: A Versatile Scaffold Endowed With Manifold Activities

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Since 1940s, Quinoxaline 1,4-dioxides (QdNO's) are known as potent antibacterial agents, and subtherapeutic levels have been used to promote growth and improve efficiency of feed conversion in animal feed. They have also shown a selective cytotoxicity against hypoxic cells present in solid tumours. Furthermore, recent studies have put in evidence that QdNO's are endowed with antitubercular, antiprotozoal and anticandida activities. On the other hand, several authors have reported about photoallergic and mutagenic effects of some derivatives. QdNO's may also cause the development of antibiotic-resistant bacteria and influence the horizontal transfer of virulence genes between bacteria.

In this review article we report the biological properties, the mode of action and Structure Activity Relationship (SAR) studies of the QdNO derivatives. Furthermore, some cytogenetic and genotoxic effects, classical and more recent method of synthesis, the quinoxaline 1,4-dioxides, and some of their most important reactions, were also reported.
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Keywords: animal growth promoting; antibacterial activity; anticandida activity; antimycobacterial activity; antiprotozoal activity; dioxides; hypoxia-selective activity; mutagenicity; quinoxaline; sar studies

Document Type: Review Article

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

Publication date: 2005-09-01

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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