On the basis of the very interesting pharmacological properties shown by the 5-amino[1,2,4]triazolo[4,3- a][1,8]naphthyridine-6-carboxamide derivatives 1, previously described by us, we have now prepared the 5-aminoimidazo[1,2-a][1,8]naphthyridine-6-carboxamide derivatives 2a–o (a new structural class) whose tricyclic system is isosteric to that of compounds 1. Both compounds 2 and some new properly substituted compounds 1 (1f–k) now synthesized were tested in vivo for their analgesic and antiinflammatory activities: on the whole, compounds 2 showed notable analgesic properties, whereas many compounds 1 exhibited a very potent anti-inflammatory activity, coupled to scarce analgesic activity. All the effective compounds proved to be completely devoid of acute gastrolesivity (gastric damage) in rats (at the 200 mg kg1 oral dose).

1,8-Naphthyridines VIII. Novel 5-aminoimidazo[1,2-a][1,8]naphthyridine-6-carboxamide and 5-amino[1,2,4]triazolo[4,3-a][1,8]naphthyridine-6-carboxamide derivatives showing potent analgesic or anti-inflammatory activity, respectively, and completely devoid of acute gastrolesivity.

DI BRACCIO, MARIO;GROSSI, GIANCARLO;
2010-01-01

Abstract

On the basis of the very interesting pharmacological properties shown by the 5-amino[1,2,4]triazolo[4,3- a][1,8]naphthyridine-6-carboxamide derivatives 1, previously described by us, we have now prepared the 5-aminoimidazo[1,2-a][1,8]naphthyridine-6-carboxamide derivatives 2a–o (a new structural class) whose tricyclic system is isosteric to that of compounds 1. Both compounds 2 and some new properly substituted compounds 1 (1f–k) now synthesized were tested in vivo for their analgesic and antiinflammatory activities: on the whole, compounds 2 showed notable analgesic properties, whereas many compounds 1 exhibited a very potent anti-inflammatory activity, coupled to scarce analgesic activity. All the effective compounds proved to be completely devoid of acute gastrolesivity (gastric damage) in rats (at the 200 mg kg1 oral dose).
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11567/225042
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