1233488-54-4Relevant articles and documents
Synthesis, vasorelaxant activity and antihypertensive effect of benzo[d]imidazole derivatives
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
experimental part, p. 3985 - 3991 (2010/08/06)
A series of 1H-benzo[d]imidazole analogues of Pimobendan, substituted at position 5 with either -CF3 or -NO2, were synthesized using a short synthetic route. All the nitro derivatives were potent, and exhibited a concentration- and partial endothelium-dependent vasorelaxant effects, with EC50s 50 value of 1.81 μM and Emax of 91.7% for ex vivo relaxant response in intact aortic rings, resulting in a 2.5-fold higher activity compared to Pimobendan. The closely related 5-CF3 analogue (compound 8), was 19 times less potent than 13. The antihypertensive activity of compound 13 was evaluated at doses of 25, 50 and 100 mg kg-1, using spontaneously hypertensive rats (SHR), showing a statistically significant dose-dependent effect.