NO-glibenclamide derivatives: Prototypes of a new class of nitric oxide-releasing anti-diabetic drugs

Endothelial dysfunction and consequent reduction of biosynthesis of endogenous nitric oxide (NO) play an important pathogenetic role in the cardiovascular complications associated with type II diabetes. In this work, the hybrid drugs 3a and 3b, nitrooxymethylbenzoate-derivatives of 1 (which is a hyd...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2009-08, Vol.17 (15), p.5426-5432
Hauptverfasser:	Calderone, Vincenzo, Rapposelli, Simona, Martelli, Alma, Digiacomo, Maria, Testai, Lara, Torri, Scilla, Marchetti, Piero, Breschi, Maria C., Balsamo, Aldo
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Aorta - drug effects Biological and medical sciences Diabetes Diabetes Mellitus, Type 2 - chemically induced Diabetes Mellitus, Type 2 - drug therapy General and cellular metabolism. Vitamins Glybenclamide Glyburide - chemistry Glyburide - pharmacology Glyburide - therapeutic use Humans Hybrid drugs Hypoglycemic Agents - chemistry Hypoglycemic Agents - pharmacology Hypoglycemic Agents - therapeutic use Insulin - metabolism Islets of Langerhans - metabolism Liver - metabolism Male Medical sciences Muscle, Smooth, Vascular - drug effects Muscle, Smooth, Vascular - metabolism Nitrates Nitric oxide Nitric Oxide - metabolism Nitric Oxide Donors - chemistry Nitric Oxide Donors - pharmacology Nitric Oxide Donors - therapeutic use Pharmacology. Drug treatments Platelet Aggregation Inhibitors - chemistry Platelet Aggregation Inhibitors - pharmacology Platelet Aggregation Inhibitors - therapeutic use Rats Rats, Wistar Sulfanylurea Vasodilator Agents - chemistry Vasodilator Agents - pharmacology Vasodilator Agents - therapeutic use
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Beschreibung
Zusammenfassung:	Endothelial dysfunction and consequent reduction of biosynthesis of endogenous nitric oxide (NO) play an important pathogenetic role in the cardiovascular complications associated with type II diabetes. In this work, the hybrid drugs 3a and 3b, nitrooxymethylbenzoate-derivatives of 1 (which is a hydroxylated active metabolite of glibenclamide 2), are reported. The pharmacodynamic characterization of 3b showed that its hypoglycaemic activity is enriched with additional NO-donor effects, conferring vasorelaxing and anti-platelet properties of potentially great usefulness for diabetes-related cardiovascular disorders.
ISSN:	0968-0896 1464-3391
DOI:	10.1016/j.bmc.2009.06.049