1,4-naphthoquinones derivatives and therapeutic use thereof

摘要

1,4 naphthoquinones derivatives, of formula (I);
wherein A is selected from the following rings:
;
their preparation and their application as antimalarial agents

主权项

1. A compound of formula (I) wherein -A is R6, which may be in position 5, 6, 7, or 8 of the phenyl ring of the naphthoquinone, represents a hydrogen atom, a halogen atom, a hydroxy group, a linear or branched (C1-C4)alkyl group, a di- or tri-fluoromethyl group, a trifluoromethoxy group, or a pentafluorosulfanyl group, n is an integer between 0 and 4, and R7 represents a methyl group; X represents —C(O)—or —CHY—, with Y being a hydrogen atom, or a hydroxy group; and R1, R2, R3, R4 and R5 each independently represent: a hydrogen atom, a halogen atom selected from the group consisting of Br, CI, and F, a hydroxy group, a methyl or t-butyl group, a di- or trifluoromethyl group, a methoxy group, a trifluoromethoxy group, —NH2, —NO2, —CN, —CONH(CH2)2CN -NHBoc, the group  and a phenyl group substituted in the para position by a t-butyl group, —NO2, —N(CH3)2, or —NHC(CH3)3, or a pharmaceutically acceptable salt of said compound, with the proviso that said compound is not