Synthesis and biological evaluation of febrifugine analogues as potential antimalarial agents
نویسندگان
چکیده
منابع مشابه
Febrifugine analogues: Promising antimalarial agents
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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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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A series of phosphoramidate and phosphorothioamidate compounds based on the lead antitubulin herbicidal agents amiprophos methyl (APM) and butamifos were synthesised and evaluated for antimalarial activity. Of these compounds, phosphorothioamidates were more active than their oxo congeners and the nature of both aryl and amido substituents influenced the desired activity. The most active compou...
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A novel series of dihydropyrimidines (DHPMs) 4a-j; 2-oxopyran-3-carboxylate 7a,b; 1-amino-1,2-dihydropyridine-3-carboxylate 8; and 1,3,4-oxadiazole derivatives 12 with quinolinyl residues have been synthesized in fairly good yields. The structure of the newly synthesized compounds was elucidated on the basis of analytical and spectral analyses. In vitro antimalarial evaluation of the synthesize...
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Background and purpose: In medicinal chemistry, molecules containing rhodanine(2-thiazolidine-4-one) ring as a magic multifunctional privileged structural and functional scaffold show a broad range of potent pharmacological properties containing anti-microbial, antiviral, anti-diabetic, and anti-convulsant effects. Evidence suggests that the activity of the rhodanine derivative correlates with ...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry
سال: 2009
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2009.05.011