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Molecular Pharmacology, Vol 20, 371-376, Copyright © 1981 by the American Society for Pharmacology and Experimental Therapeutics

Conformational Properties of Benzodioxan Derivatives with Alpha-Adrenergic Blocking Activity

ALDO BALSAMO 1, BRUNO MACCHIA 1, FRANCO MACCHIA 1, ADRIANO MARTINELLI 1, PIETRO TOGNETTI 1, and CARLO A. VERACINI 1

1 Istituto di Chimica Farmaceutica, Istituto di Chimica Organica, e Istituto di Chimica Fisica dell’Università di Pisa, 56100 Pisa Italy

Benzodioxan derivatives active on the alpha-adrenergic receptor are considered. The half-chair equilibrium of the dioxane ring was studied by 1H-NMR spectroscopy for piperoxan X and quiloflex XII. The preferred conformation was also obtained by PCILO calculations for X. The results were evaluated in order to obtain information about the mechanism of the alpha-adrenergic drug-receptor interaction.

Submitted on November 25, 1980
Accepted on May 14, 1981






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