NO-sartans: A new class of pharmacodynamic hybrids as cardiovascular drugs

被引：49

作者：

Breschi, MC

Calderone, V

Digiacomo, M

Martelli, A

Martinotti, E

Minutolo, F

Rapposelli, S

Balsamo, A

机构：

[1] Univ Pisa, Dipartimento Psichiat Neurobiol Farmacol & Biotec, I-56126 Pisa, Italy

[2] Univ Pisa, Dipartimento Sci Farmaceut, I-56126 Pisa, Italy

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2004年 / 47卷 / 23期

关键词：

D O I：

10.1021/jm049681p

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The aim of this work was to develop lead pharmacodynamic hybrids, NO-sartans, possessing the characteristics of a typical AT-antagonist and of a "slow NO donor", by adding NO-donor side chains to losartan. These new compounds, 2a and 2b, displayed vasorelaxing effects, due to the release of NO, and antagonized the vasocontractile effects of angiotensin II, with potency values similar to that of losartan. In vivo, the antihypertensive effects of 2a were similar to those of losartan and captopril.

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页码：5597 / 5600

页数：4

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