Synthesis and structure-activity relationships of phosphonic arginine mimetics as inhibitors of the M1 and M17 aminopeptidases from Plasmodium falciparum

Publikation: Beitrag in FachzeitschriftForschungsartikelBeigetragenBegutachtung


  • Komagal K Sivaraman - (Autor:in)
  • Alessandro Paiardini - (Autor:in)
  • Marcin Sieńczyk - (Autor:in)
  • Chiara Ruggeri - (Autor:in)
  • Christine A Oellig - , Monash University (Autor:in)
  • John P Dalton - (Autor:in)
  • Marcin Drag - (Autor:in)
  • Sheena McGowan - (Autor:in)


The malaria parasite Plasmodium falciparum employs two metallo-aminopeptidases, PfA-M1 and PfA-M17, which are essential for parasite survival. Compounds that inhibit the activity of either enzyme represent leads for the development of new antimalarial drugs. Here we report the synthesis and structure-activity relationships of a small library of phosphonic acid arginine mimetics that probe the S1 pocket of both enzymes and map the necessary interactions that would be important for a dual inhibitor.


Seiten (von - bis)5213-5217
FachzeitschriftJournal of Medicinal Chemistry
PublikationsstatusVeröffentlicht - Juni 2013
Extern publiziertJa

Externe IDs

Scopus 84879558016


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