PREPARATION AND ANTIPARASITIC ACTIVITY OF NEW IMIDAZOLES BEARING DIOXANE OR HEXAHYDROPYRIMIDINE MOIETY

被引：18

作者：

VANELLE, P

MALDONADO, J

CROZET, MP

SENOUKI, K

DELMAS, F

GASQUET, M

TIMONDAVID, P

机构：

[1] CNRS,URA 1412,F-13397 MARSEILLE 13,FRANCE

[2] FAC PHARM MARSEILLE,PARASITOL LAB,F-13385 MARSEILLE 5,FRANCE

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1991年 / 26卷 / 07期

关键词：

5-NITROIMIDAZOLES; 1,3-DIOXANE DERIVATIVES; HEXAHYDROPYRIMIDINE DERIVATIVES; SRN1; REACTION; ANTIPARASITIC AGENTS; AMEBICIDE ACTIVITY; TRICHOMONACIDE ACTIVITY;

D O I：

10.1016/0223-5234(91)90120-C

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

5-Nitro-1,3-dioxane and 5-nitrohexahydropyrimidine salts are found to be suitable nucleophiles for S(RN)1 reactions. From C-alkylation products, base-promoted nitrous acid elimination and acid-catalyzed cleavage of the resulting acetals afford new compounds. Only the imidazole derivatives exhibit significant amoebicide and trichomonacide activities. Structure-activity relationships are discussed.

引用

页码：709 / 714

页数：6

共 19 条

[1]

AUDIBERT P, 1979, ANN PHARM FR, V37, P483

[2]

Breccia A., 1982, NITROIMIDAZOLES CHEM

[3]

Cavier R, 1972, Bull Soc Pathol Exot Filiales, V65, P399

[4] SYNTHESIS OF NEW 5-NITROTETRAHYDRO-1,3-OXAZINE DERIVATIVES VIA ELECTRON-TRANSFER REACTIONS [J].