3 research outputs found
Antiplasmodial activity of 3-trifluoromethyl-2-carbonylquinoxaline di-N-oxide derivatives
The in vitro antiplasmodial activity of some 3-trifluoromethyl-2-carbonylquinoxaline di-N-oxide derivatives is reported. The evaluation was performed on cultures of FcB1 strain (chloroquine-resistant) of P. falciparum and the most interesting compounds were then evaluated on MCF7 tumor cells in order to evaluate an index of selectivity. The 7-methyl (2b, 4b, 5b, 6b) and nonsubstituted (3c, 4c, 5c) quinoxaline 1,4-dioxide derivatives presented the best level of activity
Unexpected reduction of ethyl 3-phenylquinoxaline-2- carboxylate 1,4-di-N-oxide derivatives by amines.
The unexpected tendency of amines and functionalized hydrazines to reduce
ethyl 3-phenylquinoxaline-2-carboxylate 1,4-di-N-oxide (1) to afford a quinoxaline 1c and
mono-oxide quinoxalines 1a and 1b is described. The experimental conditions were
standardized to the use of two equivalents of amine in ethanol under reflux for two hours,
with the aim of studying the distinct reductive profiles of the amines and the
chemoselectivity of the process. With the exception of hydrazine hydrate, which reduced
compound 1 to a 3-phenyl-2-quinoxalinecarbohydrazide derivative, the amines only acted
as reducing agents
Antiplasmodial activity of 3-trifluoromethyl-2-carbonylquinoxaline di-N-oxide derivatives
The in vitro antiplasmodial activity of some 3-trifluoromethyl-2-carbonylquinoxaline di-N-oxide derivatives is reported. The evaluation was performed on cultures of FcB1 strain (chloroquine-resistant) of P. falciparum and the most interesting compounds were then evaluated on MCF7 tumor cells in order to evaluate an index of selectivity. The 7-methyl (2b, 4b, 5b, 6b) and nonsubstituted (3c, 4c, 5c) quinoxaline 1,4-dioxide derivatives presented the best level of activity