TY - JOUR
T1 - Antileishmanial activity of quinazoline derivatives
T2 - Synthesis, docking screens, molecular dynamic simulations and electrochemical studies
AU - Mendoza-Martínez, Cesar
AU - Galindo-Sevilla, Norma
AU - Correa-Basurto, Jose
AU - Ugalde-Saldivar, Victor Manuel
AU - Rodriguez-Delgado, Rosa Georgina
AU - Hernández-Pineda, Jessica
AU - Padierna-Mota, Cecilia
AU - Flores-Alamo, Marcos
AU - Hernandez-Luis, Francisco
N1 - Publisher Copyright:
© 2014 Elsevier Masson SAS. All rights reserved.
PY - 2015/3/6
Y1 - 2015/3/6
N2 - A series of quinazoline-2,4,6-triamine were synthesized and evaluated in vitro against Leishmania mexicana. Among them, N6-(ferrocenmethyl)quinazolin-2,4,6-triamine (H2) showed activity on pro-mastigotes and intracellular amastigotes, as well as low cytotoxicity in mammalian cells. Docking and electrochemical studies showed the importance of both the ferrocene and the heterocyclic nucleus to the observed activity. H2 is readily oxidized electrochemically, indicating that the mechanism of action probably involves redox reactions.
AB - A series of quinazoline-2,4,6-triamine were synthesized and evaluated in vitro against Leishmania mexicana. Among them, N6-(ferrocenmethyl)quinazolin-2,4,6-triamine (H2) showed activity on pro-mastigotes and intracellular amastigotes, as well as low cytotoxicity in mammalian cells. Docking and electrochemical studies showed the importance of both the ferrocene and the heterocyclic nucleus to the observed activity. H2 is readily oxidized electrochemically, indicating that the mechanism of action probably involves redox reactions.
KW - Antiprotozoan activity
KW - Leishmania mexicana
KW - Quinazoline
UR - http://www.scopus.com/inward/record.url?scp=84920848098&partnerID=8YFLogxK
U2 - 10.1016/j.ejmech.2014.12.051
DO - 10.1016/j.ejmech.2014.12.051
M3 - Artículo
C2 - 25576738
SN - 0223-5234
VL - 92
SP - 314
EP - 331
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
ER -