Property activity refinement of 2-anilino 4-amino substituted quinazolines as antimalarials with fast acting asexual parasite activity
Malaria is a devastating disease caused by Plasmodium parasites. Emerging resistance
against current antimalarial therapeutics has engendered the need to develop antimalarials …
against current antimalarial therapeutics has engendered the need to develop antimalarials …
Optimization of 2-anilino 4-amino substituted quinazolines into potent antimalarial agents with oral in vivo activity
PR Gilson, C Tan, KE Jarman, KN Lowes… - Journal of medicinal …, 2017 - ACS Publications
Novel antimalarial therapeutics that target multiple stages of the parasite lifecycle are
urgently required to tackle the emerging problem of resistance with current drugs. Here, we …
urgently required to tackle the emerging problem of resistance with current drugs. Here, we …
Structural Optimization of Quinolon-4(1H)-imines as Dual-Stage Antimalarials: Toward Increased Potency and Metabolic Stability
AS Ressurreição, D Gonçalves… - Journal of Medicinal …, 2013 - ACS Publications
Discovery of novel effective and safe antimalarials has been traditionally focused on
targeting erythrocytic parasite stages that cause clinical symptoms. However, elimination of …
targeting erythrocytic parasite stages that cause clinical symptoms. However, elimination of …
Unsymmetrical Bisquinolines with High Potency against P. falciparum Malaria
KM Liebman, SJ Burgess, B Gunsaru, JX Kelly, Y Li… - Molecules, 2020 - mdpi.com
Quinoline-based scaffolds have been the mainstay of antimalarial drugs, including many
artemisinin combination therapies (ACTs), over the history of modern drug development …
artemisinin combination therapies (ACTs), over the history of modern drug development …
Optimisation of 2-(N-phenyl carboxamide) triazolopyrimidine antimalarials with moderate to slow acting erythrocytic stage activity
BL Bailey, W Nguyen, A Ngo, CD Goodman… - Bioorganic …, 2021 - Elsevier
Malaria is a devastating parasitic disease caused by parasites from the genus Plasmodium.
Therapeutic resistance has been reported against all clinically available antimalarials …
Therapeutic resistance has been reported against all clinically available antimalarials …
Antimalarial benzoheterocyclic 4-aminoquinolines: structure–activity relationship, in vivo evaluation, mechanistic and bioactivation studies
A novel class of benzoheterocyclic analogues of amodiaquine designed to avoid toxic
reactive metabolite formation was synthesized and evaluated for antiplasmodial activity …
reactive metabolite formation was synthesized and evaluated for antiplasmodial activity …
Structure–activity relationships amongst 4-position quinoline methanol antimalarials that inhibit the growth of drug sensitive and resistant strains of Plasmodium …
E Milner, W McCalmont, J Bhonsle, D Caridha… - Bioorganic & Medicinal …, 2010 - Elsevier
Utilizing mefloquine as a scaffold, a next generation quinoline methanol (NGQM) library was
constructed to identify early lead compounds that possess biological properties consistent …
constructed to identify early lead compounds that possess biological properties consistent …
Orally Bioavailable 6-Chloro-7-methoxy-4(1H)-quinolones Efficacious against Multiple Stages of Plasmodium
RM Cross, DL Flanigan, A Monastyrskyi… - Journal of Medicinal …, 2014 - ACS Publications
The continued proliferation of malaria throughout temperate and tropical regions of the world
has promoted a push for more efficacious treatments to combat the disease. Unfortunately …
has promoted a push for more efficacious treatments to combat the disease. Unfortunately …
[HTML][HTML] Parasitological profiling shows 4 (1H)-quinolone derivatives as new lead candidates for malaria
JO de Souza, SM Almeida, GE Souza, CL Zanini… - European Journal of …, 2021 - Elsevier
Abstract 4 (1H)-quinolone is an attractive template for antimalarial drug discovery
campaigns. Given the current global increase in drug and insecticide resistance, the …
campaigns. Given the current global increase in drug and insecticide resistance, the …
Design and Synthesis of Orally Bioavailable Piperazine Substituted 4(1H)-Quinolones with Potent Antimalarial Activity: Structure–Activity and Structure–Property …
R Neelarapu, JR Maignan, CL Lichorowic… - Journal of medicinal …, 2018 - ACS Publications
Malaria deaths have been decreasing over the last 10–15 years, with global mortality rates
having fallen by 47% since 2000. While the World Health Organization (WHO) recommends …
having fallen by 47% since 2000. While the World Health Organization (WHO) recommends …