5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents. Issue 22 (15th November 2016)

• Record Type: Journal Article
• Authors: 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.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 22(2016)
• Page Start: 5487
• Page End: 5491
• Publication Date: 2016-11-15
• Subjects: Plasmodium falciparum -- PfCDPK4 -- Microgametocyte exflagellation -- Malaria transmission blocking -- 5-Aminopyrazole-4-carboxamide; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.10.014
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Plasmodium falciparum calcium-dependent protein kinase 4 ( Pf CDPK4) is essential for the exflagellation of male gametocytes. Inhibition of Pf CDPK4 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 Pf CDPK4. The compounds are also able to block exflagellation of Plasmodium falciparum male gametocytes without observable toxicity to mammalian cells.