Antimalarial drug discovery: Progress and approaches

JL Siqueira-Neto, KJ Wicht, K Chibale… - Nature Reviews Drug …, 2023 - nature.com
Recent antimalarial drug discovery has been a race to produce new medicines that
overcome emerging drug resistance, whilst considering safety and improving dosing …

Towards next-generation treatment options to combat Plasmodium falciparum malaria

J Okombo, DA Fidock - Nature Reviews Microbiology, 2024 - nature.com
Malaria, which is caused by infection of red blood cells with Plasmodium parasites, can be
fatal in non-immune individuals if left untreated. The recent approval of the pre-erythrocytic …

A G358S mutation in the Plasmodium falciparum Na+ pump PfATP4 confers clinically-relevant resistance to cipargamin

D Qiu, JV Pei, JEO Rosling, V Thathy, D Li… - Nature …, 2022 - nature.com
Diverse compounds target the Plasmodium falciparum Na+ pump PfATP4, with cipargamin
and (+)-SJ733 the most clinically-advanced. In a recent clinical trial for cipargamin …

Assessing the environmental benefit of palladium-based single-atom heterogeneous catalysts for Sonogashira coupling

DF Akl, D Poier, SC D'Angelo, TP Araújo, V Tulus… - Green …, 2022 - pubs.rsc.org
The Pd–Cu catalysed Sonogashira coupling of terminal alkynes and aryl halides is a
cornerstone synthetic strategy for C–C bond formation. Homogeneous organometallic …

tRNA modification reprogramming contributes to artemisinin resistance in Plasmodium falciparum

JL Small-Saunders, A Sinha, TS Bloxham… - Nature …, 2024 - nature.com
Plasmodium falciparum artemisinin (ART) resistance is driven by mutations in kelch-like
protein 13 (PfK13). Quiescence, a key aspect of resistance, may also be regulated by a yet …

Mitigating the risk of antimalarial resistance via covalent dual-subunit inhibition of the Plasmodium proteasome

I Deni, BH Stokes, KE Ward, KJ Fairhurst… - Cell chemical …, 2023 - cell.com
The Plasmodium falciparum proteasome constitutes a promising antimalarial target, with
multiple chemotypes potently and selectively inhibiting parasite proliferation and synergizing …

Recent developments in antimalarial drug discovery

T Umumararungu, JB Nkuranga, G Habarurema… - Bioorganic & Medicinal …, 2023 - Elsevier
Although malaria remains a big burden to many countries that it threatens their socio-
economic stability, particularly in the countries where malaria is endemic, there have been …

A focus on sustainable method development for greener synthesis

JL Tyler, F Katzenburg, F Glorius - Chemical Science, 2023 - pubs.rsc.org
Given the current global climate and health challenges, sustainability and cost-effectiveness
are becoming unavoidable factors that must be considered in the development of new …

Preclinical characterization and target validation of the antimalarial pantothenamide MMV693183

LE de Vries, PAM Jansen, C Barcelo, J Munro… - Nature …, 2022 - nature.com
Drug resistance and a dire lack of transmission-blocking antimalarials hamper malaria
elimination. Here, we present the pantothenamide MMV693183 as a first-in-class acetyl …

Predicting Optimal Antimalarial Drug Combinations from a standardized Plasmodium falciparum humanized mouse model

C Demarta-Gatsi, N Andenmatten… - Antimicrobial Agents …, 2023 - Am Soc Microbiol
The development of new combinations of antimalarial drugs is urgently needed to prevent
the spread of parasites resistant to drugs in clinical use and contribute to the control and …