The development process for discovery and clinical advancement of modern antimalarials

TD Ashton, SM Devine, JJ Mohrle, B Laleu… - Journal of Medicinal …, 2019 - ACS Publications
Malaria is a devastating disease caused by Plasmodium parasites, resulting in
approximately 435000 deaths in 2018. The impact of malaria is compounded by the …

Using in Vitro Evolution and Whole Genome Analysis To Discover Next Generation Targets for Antimalarial Drug Discovery

MR Luth, P Gupta, S Ottilie… - ACS infectious diseases, 2018 - ACS Publications
Although many new anti-infectives have been discovered and developed solely using
phenotypic cellular screening and assay optimization, most researchers recognize that …

A comprehensive model for assessment of liver stage therapies targeting Plasmodium vivax and Plasmodium falciparum

A Roth, SP Maher, AJ Conway, R Ubalee… - Nature …, 2018 - nature.com
Malaria liver stages represent an ideal therapeutic target with a bottleneck in parasite load
and reduced clinical symptoms; however, current in vitro pre-erythrocytic (PE) models for …

Hydride transfer involved redox-neutral cascade cyclizations for construction of spirocyclic bisoxindoles featuring a [3, 4]-fused oxindole moiety

SS Li, S Zhu, C Chen, K Duan, Q Liu, J Xiao - Organic letters, 2019 - ACS Publications
The hydride transfer involved redox-neutral cascade cyclization has been developed to
construct the spirocyclic bisoxindoles featuring a [3, 4]-fused oxindole moiety from rationally …

Development of a Potent Inhibitor of the Plasmodium Proteasome with Reduced Mammalian Toxicity

GM LaMonte, J Almaliti, B Bibo-Verdugo… - Journal of medicinal …, 2017 - ACS Publications
Naturally derived chemical compounds are the foundation of much of our pharmacopeia,
especially in antiproliferative and anti-infective drug classes. Here, we report that a naturally …

[HTML][HTML] The early preclinical and clinical development of cipargamin (KAE609), a novel antimalarial compound

SAM Bouwman, R Zoleko-Manego, KC Renner… - Travel medicine and …, 2020 - Elsevier
Background Cipargamin (KAE609) is a novel spiroindolone class drug for the treatment of
malaria, currently undergoing phase 2 clinical development. This review provides an …

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 …

[图书][B] Parasitology: a conceptual approach

ES Loker, BV Hofkin - 2022 - taylorfrancis.com
Produced amidst the still rippling effects of a pandemic and as the world experiences the
increasing burden of global warming and a rapidly changing biosphere, the second edition …

Biochemical characterization and chemical inhibition of PfATP4-associated Na+-ATPase activity in Plasmodium falciparum membranes

JEO Rosling, MC Ridgway, RL Summers, K Kirk… - Journal of Biological …, 2018 - ASBMB
The antimalarial activity of chemically diverse compounds, including the clinical candidate
cipargamin, has been linked to the ATPase PfATP4 in the malaria-causing parasite …

Pan-active imidazolopiperazine antimalarials target the Plasmodium falciparum intracellular secretory pathway

GM LaMonte, F Rocamora, DS Marapana… - Nature …, 2020 - nature.com
A promising new compound class for treating human malaria is the imidazolopiperazines
(IZP) class. IZP compounds KAF156 (Ganaplacide) and GNF179 are effective against …