Synthesis of Lapachol and 4-Hydroxyquinazoline Derivatives as Candidates for Antimalarial Activity
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چکیده
منابع مشابه
Synthesis 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.
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چکیده ندارد.
Synthesis and antimalarial activity of novel dihydro-artemisinin derivatives.
The Plasmodium falciparum cysteine protease falcipain-2, one of the most promising targets for antimalarial drug design, plays a key role in parasite survival as a major peptide hydrolase within the hemoglobin degradation pathway. In this work, a series of novel dihydroartemisinin derivatives based on (thio)semicarbazone scaffold were designed and synthesized as potential falcipain-2 inhibitors...
متن کامل"One-pot" synthesis and antimalarial activity of formamidine derivatives of 4-anilinoquinoline.
Amodiaquine (AQ) is an antimalarial which is effective against chloroquino-resistant strains of Plasmodium falciparum but whose clinical use is severely restricted because of associated hepatotoxicity and agranulocytosis. "One-pot" synthesis of formamidines likely to be transformed into AQ derivatives is reported. Compared with AQ, the new compounds were devoid of in vitro cytotoxicity upon hum...
متن کاملSynthesis and Antimalarial Activity of Some New 3-phenyl-2- Thioxothiazolidin-4-one Derivatives
Objective: Current therapies to treat P. falciparum malaria are heavily reliant on artemisinin-based combinations. However, resistance to artemisinin has recently been identified, and resistance to key artemisinin partner drugs is already widespread. Therefore, there is an urgent need for new antimalarial drugs with improved attributes over older therapies. The objective of this research work i...
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ژورنال
عنوان ژورنال: Orbital: The Electronic Journal of Chemistry
سال: 2020
ISSN: 1984-6428
DOI: 10.17807/orbital.v12i4.1541