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.
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页码：709 / 714
页数：6
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