Abstract
The aim of this work was to develop lead pharmacodynamic hybrids, NO-sartans, possessing the characteristics of a typical AT1-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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Angiotensin II Type 1 Receptor Blockers / chemical synthesis*
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Angiotensin II Type 1 Receptor Blockers / chemistry
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Angiotensin II Type 1 Receptor Blockers / pharmacology
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Animals
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Antihypertensive Agents / chemical synthesis*
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Antihypertensive Agents / pharmacology
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Blood Pressure / drug effects
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Losartan / analogs & derivatives*
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Losartan / chemical synthesis*
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Losartan / pharmacology
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Rats
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Rats, Inbred SHR
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Structure-Activity Relationship
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Vasodilator Agents / chemical synthesis*
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Vasodilator Agents / pharmacology
Substances
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Angiotensin II Type 1 Receptor Blockers
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Antihypertensive Agents
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Vasodilator Agents
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Losartan