Mechanism-Based Design of Parasite-Targeted Artemisinin Derivatives:  Synthesis and Antimalarial Activity of Benzylamino and Alkylamino Ether Analogues of Artemisinin

Journal of Medicinal Chemistry
1996.0

Abstract

Several artemisinin derivatives linked to benzylamino and alkylamino groups were synthesized in order to enhance accumulation within the malaria parasite. The in vitro antimalarial activity was assessed against the chloroquine sensitive HB3 strain and the chloroquine resistant K1 strain of Plasmodium falciparum. In general the incorporation of amino functionality enhances the activity relative to artemisinin. The most potent analogue in the series was compound 6 which was severalfold more active than artemisinin against both strains of P. falciparum used in the study.

Knowledge Graph

Similar Paper

Mechanism-Based Design of Parasite-Targeted Artemisinin Derivatives:  Synthesis and Antimalarial Activity of Benzylamino and Alkylamino Ether Analogues of Artemisinin
Journal of Medicinal Chemistry 1996.0
Synthesis, antimalarial activity and cytotoxicity of 10-aminoethylether derivatives of artemisinin
Bioorganic & Medicinal Chemistry 2012.0
Mechanism-Based Design of Parasite-Targeted Artemisinin Derivatives:  Synthesis and Antimalarial Activity of New Diamine Containing Analogues
Journal of Medicinal Chemistry 2002.0
Structure−Activity Relationships of the Antimalarial Agent Artemisinin. 7. Direct Modification of (+)-Artemisinin and In Vivo Antimalarial Screening of New, Potential Preclinical Antimalarial Candidates
Journal of Medicinal Chemistry 2002.0
Synthesis and biological evaluation of novel quinoline-piperidine scaffolds as antiplasmodium agents
European Journal of Medicinal Chemistry 2020.0
Structure−Activity Relationships of the Antimalarial Agent Artemisinin. 8. Design, Synthesis, and CoMFA Studies toward the Development of Artemisinin-Based Drugs against Leishmaniasis and Malaria
Journal of Medicinal Chemistry 2003.0
A novel artemisinin–quinine hybrid with potent antimalarial activity
Bioorganic & Medicinal Chemistry Letters 2007.0
Potent Antimalarial Activity of Two Arenes Linked with Triamine Designed To Have Multiple Interactions with Heme
ACS Medicinal Chemistry Letters 2018.0
Synthesis of New Artemisinin Analogues from Artemisinic Acid Modified at C-3 and C-13 and Their Antimalarial Activity
Journal of Natural Products 2001.0
New 4-Aminoquinoline Mannich Base Antimalarials. 1. Effect of an Alkyl Substituent in the 5‘-Position of the 4‘-Hydroxyanilino Side Chain
Journal of Medicinal Chemistry 1999.0