Current Medicinal Chemistry

Atta-ur-Rahman, FRS
Honorary Life Fellow
Kings College
University of Cambridge


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

Author(s): A. Carta, P. Corona and M. Loriga

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


Since 1940s, Quinoxaline 1,4-dioxides (QdNOs) 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 QdNOs are endowed with antitubercular, antiprotozoal and anticandida activities. On the other hand, several authors have reported about photoallergic and mutagenic effects of some derivatives. QdNOs 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.

Keywords: quinoxaline, dioxides, animal growth promoting, antibacterial activity, hypoxia-selective activity, mutagenicity, antimycobacterial activity, anticandida activity, antiprotozoal activity, sar studies

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Article Details

Page: [2259 - 2272]
Pages: 14
DOI: 10.2174/0929867054864831
Price: $58