Febrifugine derivative antimalarial activity: quantum mechanical predictors
نویسندگان
چکیده
منابع مشابه
Febrifugine derivative antimalarial activity: quantum mechanical predictors.
Plasmodium falciparum resistant strain development has encouraged the search for new antimalarial drugs. Febrifugine is a natural substance with high activity against P. falciparum presenting strong emetic property and liver toxicity, which prevent it from being used as a clinical drug. The search for analogues that could have a better clinical performance is a current topic. We aim to investig...
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The regioisomers (2a,b) of the piperidine ring of febrifugine (1a) and isofebrifugine (1b) were synthesized from 4-allyl-3-piperidone (5). Reduction of 5 afforded a mixture of the trans and cis alcohols (6a,b) without diastereoselectivity; this result differentiated it from the reduction of 2-allyl-3-piperidone (14). The antimalarial activity of 2a,b and related compounds was tested.
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Objective: Febrifugine, a quinazoline alkaloid isolated from roots, shows powerful antimalarial Dichroa febrifuga activity against iparum. This review aimed to illustrate structural aspects of the naturally occurring Plasmodium falc febrifugine (1) and isofebrifugine (2) and how these issues were ultimately resolved by chemical synthesis. Materials and methods: Although the use of ferifugine as...
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Febrifugine is the active principal isolated 50 years ago from the Chinese herb chang shan (Dichroa febrifuga Lour), which has been used as an antimalarial in Chinese traditional medicine for more than 2,000 years. However, intensive study of the properties of febrifugine has been hindered for decades due to its side effects. We report new findings on the effects of febrifugine analogs compared...
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The subject of this thesis is the development of a potentially simple, general and economical synthetic protocol for the potent antimalarial alkaloid febrifugine (1) and its analogues. In Chapter 1, the interesting history of 1, which includes a description of several reported total syntheses of 1, is discussed. Natural products derived from 1, as well as promising synthetic derivatives that di...
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ژورنال
عنوان ژورنال: Revista do Instituto de Medicina Tropical de São Paulo
سال: 2008
ISSN: 0036-4665
DOI: 10.1590/s0036-46652008000100005