A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum-Infected Mouse Models from Structure-Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines.


:Toward improving pharmacokinetics, in vivo efficacy, and selectivity over hERG, structure-activity relationship studies around the central core of antimalarial imidazopyridazines were conducted. This study led to the identification of potent pyrazolopyridines, which showed good in vivo efficacy and pharmacokinetics profiles. The lead compounds also proved to be very potent in the parasite liver and gametocyte stages, which makes them of high interest.


J Med Chem


Le Manach C,Paquet T,Brunschwig C,Njoroge M,Han Z,Gonzàlez Cabrera D,Bashyam S,Dhinakaran R,Taylor D,Reader J,Botha M,Churchyard A,Lauterbach S,Coetzer TL,Birkholtz LM,Meister S,Winzeler EA,Waterson D,Witty MJ,Wittl




Has Abstract


2015-11-12 00:00:00












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    pub_type: 杂志文章


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    journal_title:Journal of medicinal chemistry

    pub_type: 杂志文章


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    更新日期:2020-03-12 00:00:00

  • Synthesis and biological evaluation of 4-substituted fluoronucleoside analogs for the treatment of hepatitis B virus infection.

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    journal_title:Journal of medicinal chemistry

    pub_type: 杂志文章


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    更新日期:2015-05-14 00:00:00

  • O-phenyl carbamate and phenyl urea thiiranes as selective matrix metalloproteinase-2 inhibitors that cross the blood-brain barrier.

    abstract::Brain metastasis occurs in 20-40% of cancer patients. Treatment is mostly palliative, and the inability of most drugs to penetrate the brain presents one of the greatest challenges in the development of therapeutics for brain metastasis. Matrix metalloproteinase-2 (MMP-2) plays important roles in invasion and vascular...

    journal_title:Journal of medicinal chemistry

    pub_type: 杂志文章


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    更新日期:2013-10-24 00:00:00