Synthesis and 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...
متن کاملSynthesis and characterization of analogues of the antimalarial alkaloid febrifugine
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...
متن کاملSynthesis and evaluation of phosphoramidate and phosphorothioamidate analogues of amiprophos methyl as potential antimalarial agents.
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...
متن کاملSynthesis and antimalarial activity of febrifugine derivatives.
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.
متن کاملNew Potential Antimalarial Agents: Design, Synthesis and Biological Evaluation of Some Novel Quinoline Derivatives as Antimalarial Agents.
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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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry Letters
سال: 2006
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2006.01.009