.beta.-Adrenoceptor blocking activity of halogenated thienylethanolamine derivatives

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Abstract
The synthesis of a number of ring-halogenated N-isopropyl- and N-tert-butyl-2-amino-1-(2-thienyl)ethanols was carried out to ascertain the influence of chloro or bromo substitution at the thiophene moiety on their blocking .beta.-adrenoceptor activity. Chloro- and bromo-substituted compounds exhibited a similar activity. Monohalo substitution at positions C4 or C5 of the thiophene ring resulted in comparable blocking potency; C3 halo-substituted compounds were practically devoid of activity. Animals used in potency tests were cats, rats, mice and guinea pigs. The highest activity in these series was observed with compounds dihalogenated at C4 and C5, their effect on myocardial .beta.-receptors being comparable to that of propranolol.

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