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.

Roma G; Di Braccio M; Grossi

首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >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.

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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.

机译：1,8-萘吡啶VIII。新型5-氨基咪唑（1,2-A）（1,8）萘啶-6-甲酰胺和5-氨基（1,2,4）三唑（4,3-A）（1,8）萘啶-6-甲酰胺衍生物分别显示有效的镇痛或抗炎活性，并完全没有急性胃肠栓塞。

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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 anti-inflammatory 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 kg(-1) oral dose).

机译：基于5-氨基显示的非常有趣的药理性质[1,2,4]三唑唑[4,3-a] [1,8]萘啶-6-甲酰胺衍生物1，我们有现在制备了5-aminoImidazo [1,2-a] [1,8]萘啶-6-甲酰胺衍生物2a-o（一种新的结构类），其三环系统是化合物1.化合物2和一些新的现在合成的适当取代的化合物1（1F-K）在体内进行体内进行镇痛和抗炎活动：总体上，化合物2显示出显着的镇痛性，而许多化合物1表现出非常有效的抗炎活性，偶联稀缺的镇痛活动。所有有效的化合物都证明是完全没有大鼠急性胃灭绝（胃损伤）（在200mg kg（-1）口服剂量）中。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2010年第1期|共15页
作者
Roma G; Di Braccio M; Grossi;
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Dipartimento di Scienze Farmaceutiche Universita di Genova Viale Benedetto XV 3 I-16132 Genova Italy.;

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正文语种 eng
中图分类医药、卫生;劳动卫生;
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1. 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. [J] . Roma G, Di Braccio M, Grossi European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第1期

机译：1,8-萘啶VIII。新型5-氨基咪唑并（1,2-a）（1,8）萘啶-6-羧酰胺和5-氨基（1,2,4）三唑并（4,3-a）（1,8）萘啶-6-羧酰胺衍生物分别显示出有效的镇痛或抗炎活性，并且完全没有急性胃溃疡性。
2. 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. [J] . Roma G, Di Braccio M, Grossi European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第1期

机译：1,8-萘吡啶VIII。新型5-氨基咪唑（1,2-A）（1,8）萘啶-6-甲酰胺和5-氨基（1,2,4）三唑（4,3-A）（1,8）萘啶-6-甲酰胺衍生物分别显示有效的镇痛或抗炎活性，并完全没有急性胃肠栓塞。
3. 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. [J] . Roma G, Di Braccio M, Grossi European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第1期

机译：1,8-萘吡啶VIII。新型5-氨基咪唑（1,2-A）（1,8）萘啶-6-甲酰胺和5-氨基（1,2,4）三唑（4,3-A）（1,8）萘啶-6-甲酰胺衍生物分别显示有效的镇痛或抗炎活性，并完全没有急性胃肠栓塞。
4. Pyridonecarboxylic Acids as Antibacterial Agents. VIII. Synthesis and Structure-Activity Relationship of 7-(1-Aminocyclopropyl)-4-oxo-1,8-naphthyridine-3-carboxylic Acids and 7-(1-Aminocyclopropyl)-4-oxoquinoline-3 carboxylic Acids. [O] . Yozo TODO, Jun NITTA, Mikako MIYAJIMA, 1994

机译：吡啶羧酸作为抗菌剂。 VIII。 7-（1-氨基环丙基）-4-氧代-1,8-萘啶-3-羧酸和7-（1-氨基环丙基）-4-氧代喹啉-3羧酸的合成和结构 - 活性关系。

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.

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