TY - JOUR
T1 - Flavones as isosteres of 4(1H)-quinolones
T2 - Discovery of ligand efficient and dual stage antimalarial lead compounds
AU - Rodrigues, Tiago
AU - Ressurreição, Ana S.
AU - Da Cruz, Filipa P.
AU - Albuquerque, Inês S.
AU - Gut, Jiri
AU - Carrasco, Marta P.
AU - Gonçalves, Daniel
AU - Guedes, Rita C.
AU - Dos Santos, Daniel J.V.A.
AU - Mota, Maria M.
AU - Rosenthal, Philip J.
AU - Moreira, Rui
AU - Prudêncio, Miguel
AU - Lopes, Francisca
PY - 2013
Y1 - 2013
N2 - Malaria is responsible for nearly one million deaths annually, and the increasing prevalence of multi-resistant strains of Plasmodium falciparum poses a great challenge to controlling the disease. A diverse set of flavones, isosteric to 4(1H)-quinolones, were prepared and profiled for their antiplasmodial activity against the blood stage of P. falciparum W2 strain, and the liver stage of the rodent parasite Plasmodium berghei. Ligand efficient leads were identified as dual stage antimalarials, suggesting that scaffold optimization may afford potent antiplasmodial compounds.
AB - Malaria is responsible for nearly one million deaths annually, and the increasing prevalence of multi-resistant strains of Plasmodium falciparum poses a great challenge to controlling the disease. A diverse set of flavones, isosteric to 4(1H)-quinolones, were prepared and profiled for their antiplasmodial activity against the blood stage of P. falciparum W2 strain, and the liver stage of the rodent parasite Plasmodium berghei. Ligand efficient leads were identified as dual stage antimalarials, suggesting that scaffold optimization may afford potent antiplasmodial compounds.
KW - Dual stage inhibitor
KW - Flavone
KW - Ligand efficiency
KW - Malaria
UR - http://www.scopus.com/inward/record.url?scp=84885342864&partnerID=8YFLogxK
U2 - 10.1016/j.ejmech.2013.09.008
DO - 10.1016/j.ejmech.2013.09.008
M3 - Article
C2 - 24125849
AN - SCOPUS:84885342864
SN - 0223-5234
VL - 69
SP - 872
EP - 880
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
ER -