TY - JOUR
T1 - Structure-guided lead optimization of triazolopyrimidine-ring substituents identifies potent Plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential
AU - Coteron, Jose
AU - Marco, Maria
AU - Esquivias, Jorge
AU - Deng, Xiaoyi
AU - White, Karen
AU - White, John
AU - Koltun, Maria
AU - El Mazouni, Farah
AU - Kokkonda, Sreekanth
AU - Katneni, Kasiram
AU - Bhamidipati, Ravi
AU - Shackleford, David
AU - Angulo-Barturen, Inigo
AU - Ferrer, Santiago
AU - Jimenez-Diaz, Maria Belen
AU - Gamo, Francisco-Javier
AU - Goldsmith, Elizabeth
AU - Charman, William
AU - Bathurst, Ian
AU - Floyd, David
AU - Matthews, David
AU - Burrows, Jeremy
AU - Rathod, Pradip
AU - Charman, Susan
AU - Phillips, Margaret
PY - 2011
Y1 - 2011
N2 - Drug therapy is the mainstay of antimalarial therapy, yet current
drugs are threatened by the development of resistance. In an effort to identify new potential antimalarials, we have undertaken a lead optimization program around our previously identified triazolopyrimidine-based series of Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitors.
AB - Drug therapy is the mainstay of antimalarial therapy, yet current
drugs are threatened by the development of resistance. In an effort to identify new potential antimalarials, we have undertaken a lead optimization program around our previously identified triazolopyrimidine-based series of Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitors.
UR - http://pubs.acs.org/doi/abs/10.1021/jm200592f
U2 - 10.1021/jm200592f
DO - 10.1021/jm200592f
M3 - Article
SN - 0022-2623
VL - 54
SP - 5540
EP - 5561
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 15
ER -