Synthesis and β-blocking activity of (R, S)-(E)-oximeethers of 2, 3-dihydro-1, 8-naphthyridine and 2, 3-dihydrothiopyrano [2, 3-b] pyridine: Potential antihypertensive …

…, C Manera, A Martinelli, P Nieri, G Saccomanni

Index: Ferrarini, Pier Luigi; Mori, Claudio; Badawneh, Muwaffag; Calderone, Vincenzo; Greco, Rosamiria; Manera, Clementina; Martinelli, Adriano; Nieri, Paola; Saccomanni, Giuseppe European Journal of Medicinal Chemistry, 2000 , vol. 35, # 9 p. 815 - 826

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Citation Number: 100

Abstract

The synthesis of oximeethers of 2, 3-dihydro-1, 8-naphthyridine and 2, 3-dihydrothiopyrano [2, 3-b] pyridine is described. These compounds exhibit a selective β-blocking activity, with a selectivity towards β2-receptors. Groups in the N1 position giving rise to a considerable steric hindrance led to a higher β2-blocking selectivity, whereas groups creating a moderate hindrance caused a weak but significant decrease in β2-antagonist potency. Substitution ...