5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents

Wenlin Huang, Matthew A. Hulverson, Zhongsheng Zhang, Ryan Choi, Kevin J. Hart, Mark Kennedy, Rama Subba Rao Vidadala, Dustin J. Maly, Wesley C. Van Voorhis, Scott E. Lindner, Erkang Fan, Kayode K. Ojo

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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.

Original languageEnglish (US)
Pages (from-to)5487-5491
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume26
Issue number22
DOIs
StatePublished - 2016

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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    Huang, W., Hulverson, M. A., Zhang, Z., Choi, R., Hart, K. J., Kennedy, M., Vidadala, R. S. R., Maly, D. J., Van Voorhis, W. C., Lindner, S. E., Fan, E., & Ojo, K. K. (2016). 5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents. Bioorganic and Medicinal Chemistry Letters, 26(22), 5487-5491. https://doi.org/10.1016/j.bmcl.2016.10.014