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antimalarial activity

A phase 1, placebo controlled, randomised, single ascending dose study and a volunteer infection study to characterize the safety, pharmacokinetics and antimalarial activity of the Plasmodium phosphatidylinositol 4-kinase inhibitor MMV390048

April 6, 2020 - 15:38 -- Open Access
Author(s): 
McCarthy JS, Donini C, Möhrle JJ, et al.
Reference: 
Clin Infect Dis. 2020 Apr 2. pii: ciaa368

MMV390048 is the first Plasmodium phosphatidylinositol 4-kinase inhibitor to reach clinical development as a new antimalarial. We aimed to characterize the safety, pharmacokinetics and antimalarial activity of a tablet formulation of MMV390048.

Not Open Access | Chalcone hybrids and their antimalarial activity

April 6, 2020 - 14:43 -- NOT Open Access
Author(s): 
Cheng P, Yang L, Huang X, Wang X, Gong M
Reference: 
Arch Pharm (Weinheim). 2020 Apr;353(4):e1900350

Malaria, one of the most striking, re‐emerging infectious diseases caused by the genus Plasmodium, places a huge burden on global healthcare systems. A major challenge in the control and eradication of malaria is the continuous emergence of increasingly widespread drug‐resistant malaria, creating an urgent need to develop novel antimalarial agents.

Safety, Tolerability, Pharmacokinetics, and Antimalarial Activity of the Novel Plasmodium Phosphatidylinositol 4-Kinase Inhibitor MMV390048 in Healthy Volunteers

March 30, 2020 - 10:47 -- Open Access
Author(s): 
Sinxadi P, Donini C, Johnstone H, Langdon G, Wiesner L, Allen E, Duparc S, Chalon S, McCarthy JS, Lorch U, Chibale K, Möhrle J, Barnes KI
Reference: 
Antimicrob Agents Chemother. 2020 Mar 24;64(4). pii: e01896-19

MMV390048 is a novel antimalarial compound that inhibits Plasmodium phosphatidylinositol-4-kinase. The safety, tolerability, pharmacokinetic profile, and antimalarial activity of MMV390048 were determined in healthy volunteers in three separate studies. A first-in-human, double-blind, randomized, placebo-controlled, single-ascending-dose study was performed. Additionally, a volunteer infection study investigated the antimalarial activity of MMV390048 using the Plasmodium falciparum induced blood-stage malaria (IBSM) model.

NOT Open Access | Antimalarial activity of the aqueous extract of the latex of Aloe pirottae Berger. (Aloaceae) against Plasmodium berghei in mice

March 18, 2020 - 14:57 -- NOT Open Access
Author(s): 
Dibessa TT, Engidawork E, Nedi T, Teklehaymanot T
Reference: 
J Ethnopharmacol. 2020 Mar 10:112763

In spite of worldwide efforts, malaria remains one of the most devastating illnesses in the world. The huge number of lives it takes and the resistance of malaria parasites to current drugs necessitate the search for new effective antimalarial drugs. Medicinal plants have been the major source of such drugs and A. pirottae is one of these plants used traditionally for treatment of malaria in Ethiopia.

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.

Medical Condition: 

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. 

Medical Condition: 
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