The Beirut Reaction

Haddadin, Makhluf J.; Issidorides, Costas H.

doi:10.3987/rev-92-sr(t)8

Cited by 64 publications

(34 citation statements)

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“…In 1993, Haddadin et al [113] demonstrated that QdNO compounds were photolabile in the UV region of the light spectrum, and since there, is an ample evidence that upon UV radiation these compounds produce free radicals as intermediates. They initiated the study [114] to test whether, such UV-generated intermediates interact with radicals generated in the skin following irradiation, and prevent them from exerting their harmful tumour-promoting effects [113].…”

Section: Anti-protozoal and Anti-candida Activitiesmentioning

confidence: 98%

“…They initiated the study [114] to test whether, such UV-generated intermediates interact with radicals generated in the skin following irradiation, and prevent them from exerting their harmful tumour-promoting effects [113]. The Gali-Muhtasib's team examined the ability of topical applications of QdNO's (BPQ, DCBPQ, TMQ and AMQ), which also differ in their abilities to produce photochemical intermediates, to inhibit UVB-induced ornithine decarboxylase (ODC) and DNA synthesis, and of two Trichomoniasis is a protozoan infection of the human and bovine genitourinary tracts.…”

Section: Anti-protozoal and Anti-candida Activitiesmentioning

confidence: 99%

See 1 more Smart Citation

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

Carta

Corona²,

Loriga

2005

CMC

137

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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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Section: Anti-protozoal and Anti-candida Activitiesmentioning

confidence: 98%

Section: Anti-protozoal and Anti-candida Activitiesmentioning

confidence: 99%

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

Carta

Corona²,

Loriga

2005

CMC

137

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“…Although several quinoxaline-N-oxides were evaluated as general antibacterials in the past [25][26][27] and, when considered as vitamin K analogs were even earlier suggested for possible treatment of tuberculosis [28], the systematic investigation of these agents as anitmycobacterials did not occur until the present studies. Quinoxalines and their various mono-and di-N-oxide derivatives as a class display a broad range of biological activities [25,29] and Monge and collaborators had been studying their effects in hypoxic tumor cells where aromatic N-oxides are known to undergo bioreduction [30,25].…”

Section: Quinoxaline-n-oxidesmentioning

confidence: 99%

Programs to Facilitate Tuberculosis Drug Discovery: The Tuberculosis Antimicrobial Acquisition and Coordinating Facility

Goldman

Laughon²,

Reynolds³

et al. 2007

IDDT

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There is a real need to discover new drugs that are active on drug-resistant tuberculosis (TB), and for drugs that will shorten the time of therapy. Large pharmaceutical companies have traditionally led the quest for discovering and developing new antiinfective agents but this is not the case when it comes to diseases like tuberculosis that primarily occur in resource restricted countries. Throughout the world many research groups are actively engaged in the scientific discovery of new TB drugs. Unfortunately, most research laboratories do not have the necessary safety facilities or resources for all facets of TB drug discovery. The Tuberculosis Antimicrobial Acquisition and Coordinating Facility (TAACF) was established in order to make comprehensive testing services available at no cost to research laboratories with an interest in discovering new TB drugs. The TAACF is a consortium of contracts managed and funded by the National Institute of Allergy and Infectious Diseases (National Institutes of Health, Bethesda, MD) as a resource to support preclinical drug discovery and development. The core of the TAACF is the Southern Research Institute, Birmingham, AL, which supports compound acquisition, storage, medicinal chemistry, and high throughput assays. Other collaborating groups provide biological data on antimycobacterial activity and cytotoxicity, preliminary in vivo toxicity, oral bioavailability and efficacy in animal models, specialty testing (such as activity against non-replicating persistent bacteria), and assistance in technology transfer for developing comprehensive promotional packages and facilitating partnerships with pharmaceutical companies for drug development. The TAACF program and recent progress that has been publicly disclosed by suppliers is reviewed. There are many aspects promising of the program that will not be discussed due to confidentially.

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“…[23][24][25] In our knowledge, studies related to benzofuroxan tautomerism and reactivity have not been described. On the other hand, in the preparation of phenazine N 5 ,N 10 -dioxide derivatives from benzofuroxan, [1][2][3][4][5] the effect of the benzofuroxan substituent on the isomeric proportion of the products has not been studied. 26 Herein, we present our results on the benzofuroxan tautomerism on the 1,2,5-oxadiazole-expansion process to obtain phenazine N 5 ,N 10 -dioxide derivatives.…”

Section: Introductionmentioning

confidence: 99%

“…1,2 These are obtained through an heterocycle expansion process by reaction of the corresponding 1,2,5-oxadiazole system with the phenolate carbanion generated in basic medium attacking one of the heterocyclic nitrogen ( Figure 1). When substituted benzofuroxans and phenolates are used, the reactions yield a mixture of 6-and 9-or 7-and 8-isomers.…”

Section: Introductionmentioning

confidence: 99%