scholarly journals Pharmacokinetic and Pharmacodynamic Profiles of Rapid- and Slow-Acting Antimalarial Drugs

Malaria ◽  
2019 ◽  
Author(s):  
Qigui Li ◽  
Brandon Pybus
Keyword(s):  
Antimalarial Drugs

Design, Synthesis and Antiplasmodial Evaluation of Sulfoximine-triazole Hybrids as Potential Antimalarial Prototypes

2019 ◽  
Vol 15 (6) ◽  
pp. 685-692 ◽  
Author(s):  
Tommy F. Mabasa ◽  
Babatunde Awe ◽  
Dustin Laming ◽  
Henok H. Kinfe
Keyword(s):  
Alkyl Substituent ◽  
Antimalarial Drugs ◽  
Significant Activity ◽  
Design Synthesis ◽  
Antimalarial Agents ◽  
Falciparum Strain ◽  
Physiological Properties ◽  
Resistant Strains ◽  
Cytotoxicity Activities ◽  
Drug Resistant Strains

Background:Malaria, caused by the deadly Plasmodium falciparum strain, claims the lives of millions of people annually. The emergence of drug-resistant strains of P. falciparum to the artemisinin-based combination therapy (ACT), the last line of defense against malaria, is worrisome and urges for the development of new chemo-types with a new mode of action. In the search of new antimalarial agents, hybrids of triazoles and other known antimalarial drugs have been reported to possess better activity than either of the parent compounds administered individually. Despite their better activity, no hybrid antimalarial drugs have been developed so far.Objective:In the hope of developing new antimalarial prototypes, we propose the design, synthesis and antimalarial evaluation of novel sulfoximine-triazole hybrids owing to their interesting biological and physiological properties.Methods:The sulfoximine part of the hybrid will be synthesized via imidation of the corresponding sulfoxide. Propargylation of the NH moiety of the sulfoximine followed by copper-catalyzed click chemistry with benzyl azide was envisaged to provide the target sulfoximine-triazole hybrids.Results:Five novel sulfoximine-triazole hybrids possessing various substituents on the sulfoximine moiety have been successfully synthesized and evaluated for their antiplasmodial and cytotoxicity activities. The results revealed that the co-presence of the sulfoximine and triazole moieties along with a lipophilic alkyl substituent on the sulfur atom impart significant activity.Conclusion:Sulfoximine-triazole hybrids could be used as a prototype for the synthesis of new derivatives with better antiplasmodial activities.

Induction of Haemolysis and DNA Fragmentation in a Normal and Malarial-Infected Blood by Commonly - used Antimalarial Drugs in the North-Western Region of Nigeria

2016 ◽  
Vol 10 (1) ◽  
pp. 49-55 ◽  
Author(s):  
Aliyu Muhammad ◽  
Mohammed Ibrahim ◽  
Ochuko Erukainure ◽  
Nathan Habila ◽  
Aimola Idowu ◽  
...  
Keyword(s):  
Dna Fragmentation ◽  
Antimalarial Drugs ◽  
Western Region ◽  
Infected Blood ◽  
The North ◽  
North Western

An approach to the synthesis of novel 11-hydroxyartemisinin derivatives

1991 ◽  
Vol 56 (5) ◽  
pp. 1037-1041 ◽  
Author(s):  
Orlin Petrov ◽  
Iliya Ognyanov
Keyword(s):  
Antimalarial Drugs ◽  
Artemisinin Derivatives

The conversion of artemisinin (I) to the epoxide V and its use for the preparation of novel artemisinin derivatives as potential antimalarial drugs is described.

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