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<i>β</i>-Adrenergic receptors (<i>β</i>-ARs) are G protein-coupled receptors involved in important physiological and pathological processes related to blood pressure and cardiac activity. The inhibition of cardiac <i>β</i>1-ARs could be beneficial in myocardial hypertrophy, ischemia and failure. Several carbazole-based compounds have been described as promising <i>β</i>-blockers. Herein, we investigate the capability of a carbazole derivative and three simplified indole analogs to interact with the active binding site of <i>β</i>1-AR by molecular docking studies. In the light of the obtained results, our compounds were tested by biological assays in H9c2 cardiomyocytes exposed to isoproterenol (ISO) to confirm their potential as <i>β</i>1-blockers agents, and two of them (<b>8</b> and <b>10</b>) showed interesting and promising properties. In particular, these compounds were effective against ISO-dependent in vitro cardiac hypertrophy, even at concentrations lower than the known <i>β</i>-AR antagonist propranolol. Overall, the data suggest that the indole derivatives 8 and 10 could act as potent <i>β</i>1-blockers and, active at low doses, could elicit limited side effects.