Synthesis, vasorelaxant activity and antihypertensive effect of benzo[ d]imidazole derivatives

A series of 1 H-benzo[ d]imidazole analogues of Pimobendan, substituted at position 5 with either –CF 3 or –NO 2, were synthesized using a short synthetic route. All the nitro derivatives were potent, and exhibited a concentration- and partial endothelium-dependent vasorelaxant effects, with EC 50s...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2010-06, Vol.18 (11), p.3985-3991
Hauptverfasser:	Navarrete-Vázquez, Gabriel, Hidalgo-Figueroa, Sergio, Torres-Piedra, Mariana, Vergara-Galicia, Jorge, Rivera-Leyva, Julio Cesar, Estrada-Soto, Samuel, León-Rivera, Ismael, Aguilar-Guardarrama, Berenice, Rios-Gómez, Yolanda, Villalobos-Molina, Rafael, Ibarra-Barajas, Maximiliano
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antihypertensive activity Antihypertensive agents Antihypertensive Agents - chemical synthesis Antihypertensive Agents - pharmacology Aorta - drug effects Benzimidazoles Biological and medical sciences Cardiovascular system Dose-Response Relationship, Drug Imidazoles - chemical synthesis Imidazoles - pharmacology Medical sciences Pharmacology. Drug treatments Pyridazines Rats Rats, Inbred SHR SHR Structure-Activity Relationship Vasodilator Agents - chemical synthesis Vasodilator Agents - pharmacology Vasodilator agents. Cerebral vasodilators Vasorelaxant effect
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Zusammenfassung:	A series of 1 H-benzo[ d]imidazole analogues of Pimobendan, substituted at position 5 with either –CF 3 or –NO 2, were synthesized using a short synthetic route. All the nitro derivatives were potent, and exhibited a concentration- and partial endothelium-dependent vasorelaxant effects, with EC 50s
ISSN:	0968-0896 1464-3391
DOI:	10.1016/j.bmc.2010.04.027