TY - JOUR
T1 - Synthesis and structure-activity relationships of phosphonic arginine mimetics as inhibitors of the M1 and M17 aminopeptidases from Plasmodium falciparum
AU - Kannan Sivaraman, Komagal
AU - Paiardini, Alessandro
AU - Sienczyk, Marcin
AU - Ruggeri, Chiara
AU - Oellig, Christine
AU - Dalton, John P
AU - Scammells, Peter John
AU - Drag, Marcin
AU - McGowan, Sheena
PY - 2013
Y1 - 2013
N2 - 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.
AB - 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.
UR - http://pubs.acs.org/doi/pdf/10.1021/jm4005972
U2 - 10.1021/jm4005972
DO - 10.1021/jm4005972
M3 - Article
VL - 56
SP - 5213
EP - 5217
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 12
ER -
