rka-182 and Malaria

rka-182 has been researched along with Malaria* in 4 studies

Reviews

2 review(s) available for rka-182 and Malaria

ArticleYear
Spiral molecules with antimalarial activities: A review.
    European journal of medicinal chemistry, 2022, Jul-05, Volume: 237

    Malaria is a prevalent fatal disease in tropical and subtropical regions around the world. Combinations of Artemisinin, folate antagonists, quinolines, and antibiotics are major choices in clinics. Currently, wide range of parasite's resistance necessitates the search for chemical compounds with new structures and novel antimalarial targets. The literature review was performed covering the relevant literatures published from 1966 to 2021. On the basis of structural classification (spiro-peroxides, spiroindolones, spirocyclohexadienones et al.), different types of molecules were summarized with resources, anti-malarial activities, structure-activity relationship, target introductions, resistance, development progress, and synthetic strategies, for the purpose of providing comprehensive information for developing antimalarial drugs to overcome drug resistance and highlighting the importance of the spiral structure in medicinal chemistry.

    Topics: Antimalarials; Drug Resistance; Folic Acid Antagonists; Humans; Malaria; Plasmodium falciparum; Quinolines

2022
Recent advances in malaria drug discovery.
    Bioorganic & medicinal chemistry letters, 2013, May-15, Volume: 23, Issue:10

    This digest covers some of the most relevant progress in malaria drug discovery published between 2010 and 2012. There is an urgent need to develop new antimalarial drugs. Such drugs can target the blood stage of the disease to alleviate the symptoms, the liver stage to prevent relapses, and the transmission stage to protect other humans. The pipeline for the blood stage is becoming robust, but this should not be a source of complacency, as the current therapies set a high standard. Drug discovery efforts directed towards the liver and transmission stages are in their infancy but are receiving increasing attention as targeting these stages could be instrumental in eradicating malaria.

    Topics: Animals; Antimalarials; Drug Discovery; Humans; Liver; Liver Transplantation; Malaria; Molecular Structure

2013

Other Studies

2 other study(ies) available for rka-182 and Malaria

ArticleYear
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
    Bioorganic & medicinal chemistry, 2018, 07-15, Volume: 26, Issue:11

    A series of aryl carboxamide and benzylamino dispiro 1,2,4,5-tetraoxane analogues have been designed and synthesized in a short synthetic sequence from readily available starting materials. From this series of endoperoxides, molecules with in vitro IC50s versus Plasmodium falciparum (3D7) as low as 0.84 nM were identified. Based on an assessment of blood stability and in vitro microsomal stability, N205 (10a) was selected for rodent pharmacokinetic and in vivo antimalarial efficacy studies in the mouse Plasmodium berghei and Plasmodium falciparum Pf3D70087/N9 severe combined immunodeficiency (SCID) mouse models. The results indicate that the 4-benzylamino derivatives have excellent profiles with a representative of this series, N205, an excellent starting point for further lead optimization studies.

    Topics: Administration, Oral; Animals; Antimalarials; Disease Models, Animal; Drug Stability; Humans; Inhibitory Concentration 50; Malaria; Mice; Morpholines; Plasmodium falciparum; Rats; Tetraoxanes

2018
Antimalarial mannoxanes: hybrid antimalarial drugs with outstanding oral activity profiles and a potential dual mechanism of action.
    ChemMedChem, 2011, Aug-01, Volume: 6, Issue:8

    Topics: Administration, Oral; Amodiaquine; Animals; Antimalarials; Hemeproteins; Hemin; Humans; Malaria; Mannich Bases; Mice; Molecular Dynamics Simulation; Peroxides; Phenols; Plasmodium falciparum; Spiro Compounds; Structure-Activity Relationship; Tetraoxanes

2011
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