wr-142-490 and Malaria

wr-142-490 has been researched along with Malaria* in 2 studies

Other Studies

2 other study(ies) available for wr-142-490 and Malaria

Article	Year
Design, synthesis, and characterization of novel aminoalcohol quinolines with strong in vitro antimalarial activity. European journal of medicinal chemistry, 2022, Jan-15, Volume: 228 Malaria is the fifth most lethal parasitic infections in the world. Herein, five new series of aminoalcohol quinolines including fifty-two compounds were designed, synthesized and evaluated in vitro against Pf3D7 and PfW2 strains. Among them, fourteen displayed IC Topics: Amino Alcohols; Animals; Antimalarials; Cell Line; Cricetulus; Dose-Response Relationship, Drug; Drug Design; Ether-A-Go-Go Potassium Channels; Female; Humans; Malaria; Mice; Mice, Inbred BALB C; Microsomes, Liver; Molecular Structure; Parasitic Sensitivity Tests; Plasmodium falciparum; Quinolines; Structure-Activity Relationship	2022
Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery. Science (New York, N.Y.), 2011, Dec-09, Volume: 334, Issue:6061 Most malaria drug development focuses on parasite stages detected in red blood cells, even though, to achieve eradication, next-generation drugs active against both erythrocytic and exo-erythrocytic forms would be preferable. We applied a multifactorial approach to a set of >4000 commercially available compounds with previously demonstrated blood-stage activity (median inhibitory concentration < 1 micromolar) and identified chemical scaffolds with potent activity against both forms. From this screen, we identified an imidazolopiperazine scaffold series that was highly enriched among compounds active against Plasmodium liver stages. The orally bioavailable lead imidazolopiperazine confers complete causal prophylactic protection (15 milligrams/kilogram) in rodent models of malaria and shows potent in vivo blood-stage therapeutic activity. The open-source chemical tools resulting from our effort provide starting points for future drug discovery programs, as well as opportunities for researchers to investigate the biology of exo-erythrocytic forms. Topics: Animals; Antimalarials; Cell Line, Tumor; Drug Discovery; Drug Evaluation, Preclinical; Drug Resistance; Erythrocytes; Humans; Imidazoles; Liver; Malaria; Mice; Mice, Inbred BALB C; Molecular Structure; Piperazines; Plasmodium; Plasmodium berghei; Plasmodium falciparum; Plasmodium yoelii; Polymorphism, Single Nucleotide; Protozoan Proteins; Random Allocation; Small Molecule Libraries; Sporozoites	2011

Article

Year

Design, synthesis, and characterization of novel aminoalcohol quinolines with strong in vitro antimalarial activity.

European journal of medicinal chemistry, 2022, Jan-15, Volume: 228

Malaria is the fifth most lethal parasitic infections in the world. Herein, five new series of aminoalcohol quinolines including fifty-two compounds were designed, synthesized and evaluated in vitro against Pf3D7 and PfW2 strains. Among them, fourteen displayed IC

Topics: Amino Alcohols; Animals; Antimalarials; Cell Line; Cricetulus; Dose-Response Relationship, Drug; Drug Design; Ether-A-Go-Go Potassium Channels; Female; Humans; Malaria; Mice; Mice, Inbred BALB C; Microsomes, Liver; Molecular Structure; Parasitic Sensitivity Tests; Plasmodium falciparum; Quinolines; Structure-Activity Relationship

2022

Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.

Science (New York, N.Y.), 2011, Dec-09, Volume: 334, Issue:6061

Most malaria drug development focuses on parasite stages detected in red blood cells, even though, to achieve eradication, next-generation drugs active against both erythrocytic and exo-erythrocytic forms would be preferable. We applied a multifactorial approach to a set of >4000 commercially available compounds with previously demonstrated blood-stage activity (median inhibitory concentration < 1 micromolar) and identified chemical scaffolds with potent activity against both forms. From this screen, we identified an imidazolopiperazine scaffold series that was highly enriched among compounds active against Plasmodium liver stages. The orally bioavailable lead imidazolopiperazine confers complete causal prophylactic protection (15 milligrams/kilogram) in rodent models of malaria and shows potent in vivo blood-stage therapeutic activity. The open-source chemical tools resulting from our effort provide starting points for future drug discovery programs, as well as opportunities for researchers to investigate the biology of exo-erythrocytic forms.

Topics: Animals; Antimalarials; Cell Line, Tumor; Drug Discovery; Drug Evaluation, Preclinical; Drug Resistance; Erythrocytes; Humans; Imidazoles; Liver; Malaria; Mice; Mice, Inbred BALB C; Molecular Structure; Piperazines; Plasmodium; Plasmodium berghei; Plasmodium falciparum; Plasmodium yoelii; Polymorphism, Single Nucleotide; Protozoan Proteins; Random Allocation; Small Molecule Libraries; Sporozoites

2011