A series of 1,4-dihydropyridines bearing a pharmacophoric fragment of lidoflazine was synthesized. The compounds were evaluated for inotropic, chronotropic, and calcium antagonist activities. All compounds behave as inotropic and chronotropic agents, except for compounds 4b, 5a, and 5b, which exhibit a rather weak calcium antagonism in vascular smooth muscle (like aorta). Compound 5b is about twofold more potent in decreasing both chronotropy and inotropy, while compound 5c is about fivefold more potent in decreasing inotropy than nifedipine. Moreover, compound 5b is the most potent calcium antagonist derivative of the series.
Chiarini A., Rampa A., Budriesi R., Bisi A., Fabbri G., Valenti P. (1996). 1,4-Dihydropyridine bearing a pharmacophoric fragment of lidoflazine. BIOORGANIC & MEDICINAL CHEMISTRY, 4(10), 1629-1635 [10.1016/0968-0896(96)00155-1].
1,4-Dihydropyridine bearing a pharmacophoric fragment of lidoflazine
Chiarini A.;Rampa A.;Budriesi R.;Bisi A.;Fabbri G.;Valenti P.
1996
Abstract
A series of 1,4-dihydropyridines bearing a pharmacophoric fragment of lidoflazine was synthesized. The compounds were evaluated for inotropic, chronotropic, and calcium antagonist activities. All compounds behave as inotropic and chronotropic agents, except for compounds 4b, 5a, and 5b, which exhibit a rather weak calcium antagonism in vascular smooth muscle (like aorta). Compound 5b is about twofold more potent in decreasing both chronotropy and inotropy, while compound 5c is about fivefold more potent in decreasing inotropy than nifedipine. Moreover, compound 5b is the most potent calcium antagonist derivative of the series.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
