由N-(5-降冰片-2-甲基)冰片-2-外显胺衍生的脲类和酰胺类,具有抗心律失常和其他活性。

Il Farmaco; edizione scientifica Pub Date : 1988-01-01
A Ranise, F Bondavalli, P Schenone, M Angrisani, M Lisa, R Marrazzo, E Marmo
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引用次数: 0

摘要

介绍了以樟脑亚胺与(5-降冰片烯-2-基)甲胺反应合成标题化合物,然后用NaBH4还原生成n-取代异龙脑胺(IV),再与烷基异氰酸酯、芳基异氰酸酯或酰基氯化物反应生成(IV)。一些脲类和酰胺类在大鼠中具有优于或与奎尼丁相当的抗心律失常活性,而苯甲酰胺(vo)在小鼠中表现出明显的降糖活性。此外,化合物(V)在大鼠中表现出一般的中度降压、心动过缓和抗炎活性,在小鼠中表现出弱浸润麻醉。
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Ureas and amides derived from N-(5-norbornen-2-ylmethyl) bornan-2-exo-amine with antiarrhythmic and other activities.

The synthesis of title compounds by reaction of camphor nitrimine with (5-norbornen-2-yl)methylamine, followed by NaBH4 reduction of the resulting imine to N-substituted isobornylamine (IV) and reaction of (IV) with alkyl and aryl isocyanates or acyl chlorides, is described. Some ureas and amides are endowed with antiarrhythmic activity in rats superior or comparable to that of quinidine, whereas benzamide (V o) showed an appreciable hypoglycemic activity in mice. Moreover, compounds (V) exhibited in general moderate hypotensive, bradycardic and antiinflammatory activities in rats, as well as a weak infiltration anesthesia in mice.

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