New Derivatives Of Antimalarial Drug Artemisinin

INTRODUCTION         The number people affected by malaria is channel magnitude enormously. This increasing is due to the fable drug kind variants of the sponge that ca wonts malaria the Plasmodium. This exemption is a consequence of the massive use of the quinoline-related drugs over the expiry decades. In this scenario, it became important to search for flip drugs, active against unfermented biochemical parasite targets. The drug know as artemisin or Qinghaosu (1), is a result of Chinese government campaign, to search for new active drugs against malaria, in Chinese medicinal plants. In the popular mechanism accepted for the action of artemisin, the innocent haem group, obtained during the haemoglobin digestion is proposed to catalyse the defining of oxyl radicals, by oxidation of the Fe(II) to Fe(III) and the reduction of the endoperoxide bond. These oxyl radicals rearrange in to C-centred radicals that are cytotoxic to the parasite by alkylation of snappy parasite proteins. In the experiments directed in Liverpool, the first measuring rod was to try to synthesise novel artemisin derivatives and then to do a biomimetic study, with these complicateds and the contract salt FeCl.

In the first experiment carried, it was tried to synthesise an ether (2) of the dihydroartemisin (3) and tetrazol chloride (4), development a method create by University of Algarve Organic chemical science group (see scheme 1) organization 1 In the following(a) experiments, and using a variant methodology, it was tried to synthesise, with artemisin benzoate (5) and p-trifl uoromethoxi phenol (6) as starting material,! the trifluoromethoxi phenol substituted compound (7) (see scheme 2)         Scheme 2 At last, it was d sensation a biomimetic study, reacting the obtained compound with the iron salt FeCl (scheme 3), originating two different products: the one resulting from the formation of a primary carbon centred radical (8); and from the formation of a vicarious C-centered radical (9). Scheme... If you want to get a full essay, drift it on our website: OrderCustomPaper.com

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