The past, present and future of anti-malarial medicines
Great progress has been made in recent years to reduce the high level of suffering caused
by malaria worldwide. Notably, the use of insecticide-treated mosquito nets for malaria …
by malaria worldwide. Notably, the use of insecticide-treated mosquito nets for malaria …
Antimalarial drug discovery: Progress and approaches
Recent antimalarial drug discovery has been a race to produce new medicines that
overcome emerging drug resistance, whilst considering safety and improving dosing …
overcome emerging drug resistance, whilst considering safety and improving dosing …
Structural modification aimed for improving solubility of lead compounds in early phase drug discovery
Many lead compounds fail to reach clinical trials despite being potent because of low
bioavailability attributed to their insufficient solubility making solubility a primary and crucial …
bioavailability attributed to their insufficient solubility making solubility a primary and crucial …
Quinoline‐derivatives as privileged scaffolds for medicinal and pharmaceutical chemists: A comprehensive review
The quinoline scaffolds are privileged for their numerous biological activities in the
pharmaceutical field. This moiety constitutes a well‐known space in several marketed …
pharmaceutical field. This moiety constitutes a well‐known space in several marketed …
Safety, pharmacokinetics, and antimalarial activity of the novel plasmodium eukaryotic translation elongation factor 2 inhibitor M5717: a first-in-human, randomised …
JS McCarthy, Ö Yalkinoglu, A Odedra… - The Lancet Infectious …, 2021 - thelancet.com
Background M5717 is the first plasmodium translation elongation factor 2 inhibitor to reach
clinical development as an antimalarial. We aimed to characterise the safety …
clinical development as an antimalarial. We aimed to characterise the safety …
Basic Nitrogen (BaN) is a key property of antimalarial chemical space
H Valluri, A Bhanot, S Shah, N Bhandaru… - Journal of Medicinal …, 2023 - ACS Publications
Most antimalarials are based on basic N-heterocycles and possess amine functionalities.
Despite this, the role of basic nitrogen (BaN) in antimalarial drug design has not been …
Despite this, the role of basic nitrogen (BaN) in antimalarial drug design has not been …
Screening the medicines for malaria venture pathogen box across multiple pathogens reclassifies starting points for open-source drug discovery
Open-access drug discovery provides a substantial resource for diseases primarily affecting
the poor and disadvantaged. The open-access Pathogen Box collection is comprised of …
the poor and disadvantaged. The open-access Pathogen Box collection is comprised of …
High-throughput screening platform to identify inhibitors of protein synthesis with potential for the treatment of malaria
F Tamaki, F Fisher, R Milne, FSR Terán… - Antimicrobial Agents …, 2022 - Am Soc Microbiol
Artemisinin-based combination therapies have been crucial in driving down the global
burden of malaria, the world's largest parasitic killer. However, their efficacy is now …
burden of malaria, the world's largest parasitic killer. However, their efficacy is now …
Antimalarial drug discovery: from quinine to the most recent promising clinical drug candidates
C Tisnerat, A Dassonville-Klimpt… - Current Medicinal …, 2022 - ingentaconnect.com
Malaria is a tropical threatening disease caused by Plasmodium parasites, resulting in
409,000 deaths in 2019. The delay of mortality and morbidity has been compounded by the …
409,000 deaths in 2019. The delay of mortality and morbidity has been compounded by the …
New quinoline/chalcone hybrids as anti-cancer agents: Design, synthesis, and evaluations of cytotoxicity and PI3K inhibitory activity
A series of quinoline-chalcone hybrids was designed as potential anti-cancer agents,
synthesized and evaluated. Different cytotoxic assays revealed that compounds …
synthesized and evaluated. Different cytotoxic assays revealed that compounds …