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

被引：33

作者：

MONGE, A ^{[1
]}

ALDANA, I ^{[1
]}

ALVAREZ, T ^{[1
]}

FONT, M ^{[1
]}

SANTIAGO, E ^{[1
]}

LATRE, JA ^{[1
]}

BERMEJILLO, MJ ^{[1
]}

LOPEZUNZU, MJ ^{[1
]}

FERNANDEZALVAREZ, E ^{[1
]}

机构：

[1] CTR NACL QUIM ORGAN,E-28006 MADRID,SPAIN

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1991年 / 34卷 / 10期

关键词：

D O I：

10.1021/jm00114a010

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Some fused 5H-pyridazino[4,5-b]indoles (7-10), substituted in positions 1 and 4 by hydrazine and/or amino groups, have been synthesized. These new compounds present a planar topography, a dipole with an adjacent acidic proton, and a basic hydrogen-acceptor site opposite the dipole. These compounds have some resemblance to carbazeram and other pyridazino agents with cardiotonic activity. Some of the new compounds here described possess inotropic activity (Table I and II), with a complementary effect as inhibitors of platelet aggregation (Tables III and IV). 1-Hydrazino-4-(3,5-dimethyl)-1-pyrazolyl-5H-pyridazino[4,5-b]indole hydrochloride (7a.HCl) is the first compound described in the literature with activities as inhibitor of PDE-IV and as selective inhibitor of TXA2 synthetase (Table V).

引用

页码：3023 / 3029

页数：7

共 32 条

[1] CARDIOTONIC ACTIVITY OF MILRINONE, A NEW AND POTENT CARDIAC BIPYRIDINE, ON THE NORMAL AND FAILING HEART OF EXPERIMENTAL-ANIMALS [J].