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antimalarial activity

NOT Open Access | Discovery of 6'-chloro-N-methyl-5'-(phenylsulfonamido)-[3,3'-bipyridine]-5-carboxamide (CHMFL-PI4K-127) as a novel Plasmodium falciparum PI(4)K inhibitor with potent antimalarial activity against both blood and liver stages of Plasmodium

January 14, 2020 - 12:02 -- NOT Open Access
Author(s): 
Liang X, Jiang Z, Liu Q, et al.
Reference: 
European Journal of Medicinal Chemistry, Volume 188, 15 February 2020, 112012

Starting from a bipyridine-sulfonamide scaffold, medicinal chemistry optimization leads to the discovery of a novel Plasmodium falciparum PI4K kinase (PfPI4K) inhibitor compound 15g (CHMFL-PI4K-127, IC50: 0.9 nM), which exhibits potent activity against 3D7 Plasmodium falciparum (P. falciparum) (EC50: 25.1 nM). CHMFL-PI4K-127 displays high selectivity against PfPI4K over human lipid and protein kinase.

Antimalarial activity of hydromethanolic extract and its solvent fractions of Vernonia amygdalina leaves in mice infected with Plasmodium berghei

November 26, 2019 - 20:40 -- Open Access
Author(s): 
Temesgen Bihonegn, Mirutse Giday, Getnet Yimer, Abebe Animut, Mekonnen Sisay
Reference: 
SAGE Open Medicine Volume 7: 1–10

Vernonia amygdalina Del. (Asteraceae) is reported to be traditionally used for the treatment of malaria. Based on folkloric repute of this plant in Ethiopian traditional medicine and crude extract-based ethnopharmacological studies conducted in few countries, this study was undertaken to evaluate the in vivo antimalarial activity of 80% methanol extract and its solvent fractions of the leaves of V. amygdalina in mice infected with Plasmodium berghei.

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Current scenario of ferrocene-containing hybrids for antimalarial activity

November 8, 2019 - 17:02 -- Open Access
Author(s): 
Xiao J, Sun Z, Kong F, Gao F.
Reference: 
Eur J Med Chem. 2019 Oct 17; 185:111791

Hybrid molecules have the potential to enhance the efficacy against both drug-sensitive and drug-resistant organisms, and Ferroquine, a ferrocene hybrid, has demonstrated great potency in clinical trials against both drug-sensitive and drug-resistant malaria. Accordingly, hybridization of ferrocene with other antimalarial pharmacophores represents a promising strategy to develop novel antimalarial candidates.

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A single dose combination study with the experimental antimalarials artefenomel and DSM265 to determine safety and antimalarial activity against blood-stage Plasmodium falciparum in healthy volunteers

November 8, 2019 - 16:44 -- Open Access
Author(s): 
McCarthy J, Rückle T, Elliott SL, Ballard E, Collins KA, Marquart L, Griffin P, Chalon S, Möhrle JJ
Reference: 
Antimicrob Agents Chemother. 2019 Nov 4

Artefenomel and DSM265 are two new compounds that have been shown to be well tolerated and effective when administered as monotherapy malaria treatment. This study aimed to determine the safety, pharmacokinetics and pharmacodynamics of artefenomel and DSM265 administered in combination to healthy subjects in a volunteer infection study using the Plasmodium falciparum induced blood stage malaria model. 

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