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5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents.
Huang, Wenlin; Hulverson, Matthew A; Zhang, Zhongsheng; Choi, Ryan; Hart, Kevin J; Kennedy, Mark; Vidadala, Rama Subba Rao; Maly, Dustin J; Van Voorhis, Wesley C; Lindner, Scott E; Fan, Erkang; Ojo, Kayode K.
Afiliação
  • Huang W; Department of Biochemistry, University of Washington, Seattle, WA 98195, United States.
  • Hulverson MA; Division of Allergy & Infectious Disease, Center for Emerging & Reemerging Infectious Disease (CERID), University of Washington, Seattle, WA 98109, USA.
  • Zhang Z; Department of Biochemistry, University of Washington, Seattle, WA 98195, United States.
  • Choi R; Division of Allergy & Infectious Disease, Center for Emerging & Reemerging Infectious Disease (CERID), University of Washington, Seattle, WA 98109, USA.
  • Hart KJ; Department of Biochemistry and Molecular Biology, Center for Malaria Research, Pennsylvania State University, PA 16802, USA.
  • Kennedy M; Department of Biochemistry and Molecular Biology, Center for Malaria Research, Pennsylvania State University, PA 16802, USA.
  • Vidadala RSR; Department of Chemistry, University of Washington, Seattle, WA 98195, USA.
  • Maly DJ; Department of Biochemistry, University of Washington, Seattle, WA 98195, United States; Department of Chemistry, University of Washington, Seattle, WA 98195, USA.
  • Van Voorhis WC; Division of Allergy & Infectious Disease, Center for Emerging & Reemerging Infectious Disease (CERID), University of Washington, Seattle, WA 98109, USA. Electronic address: wesley@uw.edu.
  • Lindner SE; Department of Biochemistry and Molecular Biology, Center for Malaria Research, Pennsylvania State University, PA 16802, USA.
  • Fan E; Department of Biochemistry, University of Washington, Seattle, WA 98195, United States. Electronic address: erkang@u.washington.edu.
  • Ojo KK; Division of Allergy & Infectious Disease, Center for Emerging & Reemerging Infectious Disease (CERID), University of Washington, Seattle, WA 98109, USA. Electronic address: ojo67kk@u.washington.edu.
Bioorg Med Chem Lett ; 26(22): 5487-5491, 2016 11 15.
Article em En | MEDLINE | ID: mdl-27780638
ABSTRACT
Plasmodium falciparum calcium-dependent protein kinase 4 (PfCDPK4) is essential for the exflagellation of male gametocytes. Inhibition of PfCDPK4 is an effective way of blocking the transmission of malaria by mosquitoes. A series of 5-aminopyrazole-4-carboxamide analogues are demonstrated to be potent inhibitors of PfCDPK4. The compounds are also able to block exflagellation of Plasmodium falciparum male gametocytes without observable toxicity to mammalian cells.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Plasmodium falciparum / Proteínas Quinases / Pirazóis / Antimaláricos Limite: Animals / Humans / Male Idioma: En Ano de publicação: 2016 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Plasmodium falciparum / Proteínas Quinases / Pirazóis / Antimaláricos Limite: Animals / Humans / Male Idioma: En Ano de publicação: 2016 Tipo de documento: Article