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antimalarial activity

Enhancing the antimalarial activity of artesunate

July 8, 2020 - 15:55 -- Open Access
Adebayo JO, Tijjani H, Adegunloye AP, Ishola AA, Balogun EA, Malomo SO
Parasitol Res. 2020 Jul 7

The global challenge to the treatment of malaria is mainly the occurrence of resistance of malaria parasites to conventionally used antimalarials. Artesunate, a semisynthetic artemisinin compound, and other artemisinin derivatives are currently used in combination with selected active antimalarial drugs in order to prevent or delay the emergence of resistance to artemisinin derivatives.

NOT Open Access | Total Synthesis and Antimalarial Activity of Dominicin, a Cyclic Octapeptide from a Marine Sponge

June 3, 2020 - 07:01 -- NOT Open Access
Bérubé C, Borgia A, Gagnon D, Mukherjee A, Richard D, Voyer N
J Nat Prod. 2020 Jun 2

Dominicin, a macrocyclic peptide isolated from the marine sponge Eurypon laughlini, has been synthesized for the first time by solid-phase peptide synthesis. The strategy uses oxime resin and takes advantage of the nucleophile susceptibility of the oxime ester bond.

Antimalarial activity of artefenomel against asexual parasites and transmissible gametocytes during experimental blood-stage Plasmodium vivax infection

June 2, 2020 - 09:34 -- Open Access
Collins KA, Abd-Rahman AN, Marquart L, Ballard E, Gobeau N, Griffin P, Chalon S, Möhrle JJ, McCarthy JS
J Infect Dis. 2020 Jun 1:jiaa287

Interventions that effectively target Plasmodium vivax are critical for the future control and elimination of malaria. We conducted a P. vivax volunteer infection study to characterise the antimalarial activity of artefenomel, a new drug candidate.

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
McCarthy JS, Donini C, Möhrle JJ, et al.
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
Cheng P, Yang L, Huang X, Wang X, Gong M
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
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
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
Dibessa TT, Engidawork E, Nedi T, Teklehaymanot T
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
Liang X, Jiang Z, Liu Q, et al.
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
Temesgen Bihonegn, Mirutse Giday, Getnet Yimer, Abebe Animut, Mekonnen Sisay
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.


Current scenario of ferrocene-containing hybrids for antimalarial activity

November 8, 2019 - 17:02 -- Open Access
Xiao J, Sun Z, Kong F, Gao F.
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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