Carbazole and Simplified Derivatives: Novel Tools toward β-Adrenergic Receptors Targeting

نویسندگان

چکیده

β-Adrenergic receptors (β-ARs) are G protein-coupled involved in important physiological and pathological processes related to blood pressure cardiac activity. The inhibition of β1-ARs could be beneficial myocardial hypertrophy, ischemia failure. Several carbazole-based compounds have been described as promising β-blockers. Herein, we investigate the capability a carbazole derivative three simplified indole analogs interact with active binding site β1-AR by molecular docking studies. In light obtained results, our were tested biological assays H9c2 cardiomyocytes exposed isoproterenol (ISO) confirm their potential β1-blockers agents, two them (8 10) showed interesting properties. particular, these effective against ISO-dependent vitro even at concentrations lower than known β-AR antagonist propranolol. Overall, data suggest that derivatives 8 10 act potent and, low doses, elicit limited side effects.

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ژورنال

عنوان ژورنال: Applied sciences

سال: 2021

ISSN: ['2076-3417']

DOI: https://doi.org/10.3390/app11125486