Fexinidazole, a DNA synthesis inhibitor, is being developed by Drugs for Neglected Diseases initiative (DNDi), in collaboration with Sanofi for the oral.
Fexinidazole is a medication used to treat African trypanosomiasis (sleeping sickness) cause by Trypanosoma brucei gambiense. It is effective against both first and second stage disease. Some evidence also supports its use in Chagas disease. It is taken by mouth. Common side effects include nausea, vomiting, headache, and trouble sleeping. Other side effects may include QT prolongation.Fexinidazole (Fxn) is a 2-substituted 5-nitroimidazole (Fig. 3) with potent anti-T. brucei activity 177 that was rediscovered as a hit upon screening of a nitroheterocyclics library. 178,179 Based on the common active nitro group, the antitrypanosomal mode of action of Fxn is assumed to be similar to that described for Nfx and Bzn. The biological activity of Fxn against infective T. brucei (EC.Fexinidazole Winthrop will be available as 600- mg tablets. The active substance of Fexinidazole Winthrop is fexinidazole, a nitro-imidazole derivative that generates reactive amines that exert indirect toxic and mutagenic effects on the trypanosomes.
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Imidazole is an entity which has interesting physical and chemical properties, in the present article focus lies on analysis of these properties which in turn may be exploited for different pharmacological activities, like compounds having a 3,4,5-trimethoxyphenyl ring linked to either N-1 or C-4 position of the imidazole entity gave an interesting profile of cytotoxicity with specific.
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Molecules 2009, 14 2433 ethyl)-2-nitro-1H-imidazol-5-carboxylic acid (3) (9) which was readily prepared via oxidation of the CH3 group of compound 2, was converted into acid chloride 4 through reaction with thionyl chloride. The structures of compounds 3 and 4 were confirmed by 1H-NMR and IR spectral data and elemental analysis. In the IR spectrum compound 3 the presence of an OH absorption at.
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Fexinidazole has been investigated for the treatment of Disease, Chagas and South American Trypanosomiasis.
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Additionally, the synthesis of a 14 C-labeled version of fexinidazole for absorption, distribution, metabolism, and excretion studies is also described via a five-step procedure starting from.
Our findings show that oral fexinidazole is effective and safe for the treatment of T b gambiense infection compared with nifurtimox eflornithine combination therapy in late-stage HAT patients. Fexinidazole could be a key asset in the elimination of this fatal neglected disease.
P. N. Gaponik, O. A. Ivashkevich TETRAZOLES: SYNTHESIS, STRUCTURES, PHYSICO-CHEMICAL PROPERTIES AND APPLICATION INTRODUCTION The paper represents a brief review of works published by the authors over a pe- riod of 1980-2003 years in the field of synthesis and investigations of proper-.
Imidazole and Benzimidazole Synthesis is a comprehensive survey of the known methods of syntheses and ring modification. It brings together the multitude of synthesis of the imidazole ring in a systemic way interms of specific bond formation, and recommends the most attractive synthetic approaches.
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