Abstract
Quinoxaline 1,4-di-N-oxides (QdNOs) have manifold biological properties, including antimicrobial, antitumoral, antitrypanosomal and antiinflammatory/antioxidant activities. These diverse activities endow them broad applications and prospects in human and veterinary medicines. As QdNOs arouse widespread interest, the evaluation of their medicinal chemistry is still in progress. In the meantime, adverse effects have been reported in some of the QdNO derivatives. For example, genotoxicity and bacterial resistance have been found in QdNO antibacterial growth promoters, conferring urgent need for discovery of new QdNO drugs. However, the modes of actions of QdNOs are not fully understood, hindering the development and innovation of these promising compounds. Here, QdNOs are categorized based on the activities and usages, among which the antimicrobial activities are consist of antibacterial, antimycobacterial and anticandida activities, and the antiprotozoal activities include antitrypanosomal, antimalarial, antitrichomonas, and antiamoebic activities. The structure-activity relationship and the mode of actions of each type of activity of QdNOs are summarized, and the toxicity and the underlying mechanisms are also discussed, providing insight for the future research and development of these fascinating compounds.
Highlights
Quinoxaline is a heterocyclic compound containing a benzene ring and a pyrazine ring
The QdNO antibacterial growth promoters have been widely used as feed additives to prevent infectious disease and improve animal growth since 1970s (Carta et al, 2005), and the antitumoral drug, TPZ (3-amino-BTO 1,4 dioxide, SR4233), has been subjected to phase topoisomerase II (II) clinical trial (Covens et al, 2006; Maluf et al, 2006; Cohen et al, 2007)
The antibacterial activity of QdNOs was first reported in McIlwain (1943), and subtherapeutic levels of antibacterial QdNOs have been used for nearly 50 years to promote the growth of animals and improve efficiency of feed conversion in animal husbandry (Carta et al, 2005)
Summary
Quinoxaline is a heterocyclic compound containing a benzene ring and a pyrazine ring Oxidation of both nitrogens of the pyrazine ring to obtain QdNO offers it variety of biological properties, including antitumoral, antibacterial, anticandida, antitrypanosomal, antiinflammatory/ antioxidant, and mutagenic properties. With the wide use of QdNOs, the toxicity and drug resistance gradually have become the disadvantages for further application of these promising compounds. The study of SAR combined with the study of drug action will explain the reason for that different structures of QdNOs exhibit different activities. The mode of actions of QdNOs and the SAR analysis are elucidated and updated in sort of the different biological properties, giving insight to the future development of these fascinating compounds
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