Enantiomers of 8-(3-tert-Butylamino-2-hydroxypropoxy)-3,4-dihydro-3-oxo-2H-(1,4)benzothiazine: Racemic Resolution, Chiral Synthesis and Biological Activity

Autor:	Schiaffella, F., Fringuelli, R., Violetta Cecchetti, Fravolini, A., Angeli, P., Marucci, G.
Jazyk:	angličtina
Rok vydání:	1990
Předmět:	Male Magnetic Resonance Spectroscopy Adrenergic beta-Antagonists Guinea Pigs Thiazines Muscle Smooth Stereoisomerism In Vitro Techniques Myocardial Contraction Electric Stimulation Rats Trachea Vas Deferens Animals Carteolol Adrenergic alpha-Antagonists Muscle Contraction
Zdroj:	Scopus-Elsevier
Popis:	We report the resolution of racemic (+/-)-1 with (R)-(+)-methylbenzyl isocianate and the synthesis of (R)-1 and (S)-1 via Sharpless chiral epoxidation. The enantio- and tissue-selectivity of such enantiomers, as beta- and alpha-adrenoceptor antagonists, were studied. Compound 1, while confirming the potent beta-blocking activity, displayed a modest enantio-selectivity towards beta 1- and beta 2-adrenoceptors. All the compounds displayed no activity as alpha-adrenoceptor blockers.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=pmid_dedup__::3d98ba7aad620c7842426ce6e6adf5bd http://hdl.handle.net/11391/909539 Zobrazit plný text záznamu