NEW INDOLE AND TRIAZINO[5,4-B]INDOL-4-ONE DERIVATIVES - SYNTHESIS AND STUDIES AS INOTROPICS AND INHIBITORS OF BLOOD-PLATELET AGGREGATION

被引：5

作者：

MONGE, A ^{[1
]}

ALDANA, I ^{[1
]}

FONT, M ^{[1
]}

ARRARAS, JA ^{[1
]}

SANTIAGO, E ^{[1
]}

LOPEZUNZU, MJ ^{[1
]}

MARTINEZDEIRUJO, JJ ^{[1
]}

ALBERDI, E ^{[1
]}

FERNANDEZALVAREZ, E ^{[1
]}

机构：

[1] NATL CTR ORGAN CHEM, E-28006 MADRID, SPAIN

来源：

ARCHIV DER PHARMAZIE | 1992年 / 325卷 / 07期

关键词：

D O I：

10.1002/ardp.19923250712

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

New triazino[5,4-b]indol-4-one derivatives carrying amino groups in position 3 were synthetized and tested as inotropic agents and inhibitors of platelet aggregation. 2h, 2p, 5p, and 6g are the most active as inotropic agents. Compounds were tested as inhibitors of platelet aggregation induced by adenosine 5'-diphosphate (ADP) and arachidonic acid (AA) (guinea pig whole blood). 2k, 2p, 5o, 6d, 6m, and 6o are the most active as inhibitors of the platelet aggregation induced by AA. 6d, 6h, and 6o are most active compounds also in the aggregation induced by ADP. Radioimmunoassay studies, following AA induced aggregation, measuring thromboxane B2 (TXB2) and prostaglandin E2 (PGE2) were carried out on compounds 2b, 2d, 2f, 2g, 2h, 2i, 2k, 2m, 2o, 2p, 2r, 5i, 5j, 5k, 5r, and 5f, which inhibit platelet aggregation induced by AA. None of the compounds tested turned out to be selective inhibitors. Compounds 2h and 2p showed both inotropic and platelet aggregation inhibiting activity.

引用

页码：439 / 452

页数：14

共 32 条

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