NO-Sartans: A New Class of Pharmacodynamic Hybrids as Cardiovascular Drugs

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...

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Veröffentlicht in:	Journal of medicinal chemistry 2004-11, Vol.47 (23), p.5597-5600
Hauptverfasser:	Breschi, Maria C, Calderone, Vincenzo, Digiacomo, Maria, Martelli, Alma, Martinotti, Enrica, Minutolo, Filippo, Rapposelli, Simona, Balsamo, Aldo
Format:	Artikel
Sprache:	eng
Schlagworte:	Angiotensin II Type 1 Receptor Blockers - chemical synthesis Angiotensin II Type 1 Receptor Blockers - chemistry Angiotensin II Type 1 Receptor Blockers - pharmacology Animals Antihypertensive agents Antihypertensive Agents - chemical synthesis Antihypertensive Agents - pharmacology Biological and medical sciences Blood Pressure - drug effects Cardiovascular system Losartan - analogs & derivatives Losartan - chemical synthesis Losartan - pharmacology Medical sciences Pharmacology. Drug treatments Rats Rats, Inbred SHR Structure-Activity Relationship Vasodilator Agents - chemical synthesis Vasodilator Agents - pharmacology
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Zusammenfassung:	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.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm049681p