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Synthesis and beta-adrenergic blocking activity of oxipropanolamines of 3,4-dihydro-3-oxo-2H(1,4)benzothiazine
Authors:V Cecchetti  A Fravolini  R Fringuelli  F Schiaffella  G Mascellani  P G Pagella  P L Rugarli
Affiliation:Istituto di Chimica Farmaceutica e Tecnica Farmaceutica-Università di Perugia, Italy.
Abstract:The synthesis of a series of oxypropanolamines of 3,4-dihydro-3-oxo-2H(1,4)benzothiazine is reported. Some of these compounds proved more potent than propranolol and carteolol as beta-adrenergic blocking agents in in vitro tests. The 8-(3-tert-butylamino-2-hydroxy)propoxy-3,4-dihydro-3-oxo-2H(1,4) benzothiazine fumarate (XVI a), which gave better results, confirmed its remarkable activity in in vivo tests.
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