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ID: ALA3864161

Journal: Bioorg Med Chem Lett

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

Authors: Huang W, Hulverson MA, Zhang Z, Choi R, Hart KJ, Kennedy M, Vidadala RSR, Maly DJ, Van Voorhis WC, Lindner SE, Fan E, Ojo KK.

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.

CiteXplore: 27780638

DOI: 10.1016/j.bmcl.2016.10.014