| 摘要 |
The present invention refers to new compounds derived from artesunate salts with quinolines represented by the general formula (I) where X is represented by the general formula (II) and Y is represented by the general formula (III) depending on the radicals substituted in X (formula II), the relation X to Y (formula III) may vary from 1:1 to 1:7, because the amount of Y depends on the amount of N available in X for the formation of the salt. The radicals R1, R2, R3, R4, R5, e R6 in the general formula (II) are represented by: R1═H, CF3, CH3, OCH3, NH2, halogen; R2═H, CH3, NH2, halogen, NH—CHCH3(CH2)3N(C2H5)(CH2CH2OH), CH(OH)-2(C5H11N), NH—R7—N—(C2H5)2; R3═H, m-OC6H4CF3, NH2; R4═H, CH3, OCH3, NH2, halogen; R5═H, CH3, CF3, NH2, halogen; R6═H, CF3, CH3, NH2, halogen, NH—R8—N—(C2H5)2, NHCH(CH3)(CH2)3NH2; R7═(CH2)2, (CH2)3, CHCH3CH2, (CH2)4, (CH2)5, CHCH3(CH2)3(CH2)6, (CH2)8, (CH2)10, (CH2)12; R8═CHCH3(CH2)3, CHCH3(CH2)CHCH3, (CH2)2, (CH2)3, (CH2)6, (CH2)3O(CH2)3. The present invention also refers to a process of preparation of these general formula (I) compounds, and the pharmaceutical compositions, in which these compounds are included especially their use as medicine for treatment or prevention or inhibition of malaria or other parasitic diseases such as: kaodzera, Chagas disease, leishmaniasis, amoebiasis, giardiasis, trichommoniasis, toxoplasmosis, schistosomiasis, as well as other helminthiases. |
