AMINOACYLATES AND AMINOCARBAMATES OF 2-SUBSTITUTED 4-HYDROXYMETHYL-1,3-DIOXOLANS AS AMMONIUM-SALTS - A NEW SERIES OF PAF ANTAGONISTS

被引：4

作者：

BROQUET, C ^{[1
]}

AUCLAIR, E ^{[1
]}

BLAVET, N ^{[1
]}

TOUVAY, C ^{[1
]}

BRAQUET, P ^{[1
]}

机构：

[1] INST H BEAUFOUR,F-92350 LE PLESSIS ROBINS,FRANCE

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1990年 / 25卷 / 03期

关键词：

aggregation; bronchoconstriction; leukopenia; PAF antagonists; synthesis; thrombocytopenia;

D O I：

10.1016/0223-5234(90)90206-I

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and biological activity of some aminoacylate and aminocarbamate ammonium salts of 2-substituted 4-hydroxymethyl 1,3-dioxolans are described. The compounds were obtained as mixtures of diastereoisomeric racemates. In vitro, platelet aggregation (PRP) induced by PAF was antagonized by all derivatives. In vivo (in the guinea pig, iv), the PAF-induced bronchoconstriction, thrombocytopenia and leukopenia, were inhibited by most of them. Among the synthesized compounds, two highly potent and specific PAF antagonists: BN 52111 and BN 52115 have been identified. © 1990.

引用

页码：235 / 240

页数：6

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