INVIVO AND INVITRO EFFECTS OF METHACRYLANILIDES AND ACETYLCARBOXANILIDE ON ALKALINE-PHOSPHATASE ACTIVITY OF ECHINOCOCCUS-MULTILOCULARIS METACESTODES

被引：1
作者：
AUDIN, P
SARCIRON, ME
PARIS, J
PETAVY, AF
机构：
[1] Groupe de Recherches sur les Antiparasitaires, Faculté de Pharmacie, 69373 Lyon Cedex 08
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1992年 / 27卷 / 03期
关键词：
ECHINOCOCCUS-MULTILOCULARIS; ALKALINE PHOSPHATASE; SYNTHETIC INHIBITORS; ANILIDES;
D O I：
10.1016/0223-5234(92)90013-Q
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
In our search for effective chemotherapy of alveolar hydatid disease we are investigating key enzymes of Echinococcus multilocularis metacestodes. Isatin (2,3-indolinedione) is well known as an inhibitor of alkaline phosphatase activity, and has been previously investigated. Acetylcarboxanilide, an 'open drug' of isatin and 2 methacrylanilides were evaluated for their ability to inhibit alkaline phosphatase activity of Echinococcus multilocularis metacestodes in vivo. These 'open drugs' are more efficient than isatin, and para-chloromethacrylanilide exhibits a strong selectivity for the parasite enzyme and is also effective in vitro. The results obtained with para-chloromethacrylanilide are promising.
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收藏
页码：285 / 289
页数：5
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