1,8-Naphthyridines VI. Synthesis and anti-inflammatory activity of 5-(alkylamino)-N,N-diethyl(1,2,4)triazolo(4,3-a)(1,8)naphthyridine-6-carboxamides with a new substitution pattern on the triazole ring.

Di-Braccio M; Grossi G; Roma G; Piras D; Mattioli F; Gosmar M

首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >1,8-Naphthyridines VI. Synthesis and anti-inflammatory activity of 5-(alkylamino)-N,N-diethyl(1,2,4)triazolo(4,3-a)(1,8)naphthyridine-6-carboxamides with a new substitution pattern on the triazole ring.

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1,8-Naphthyridines VI. Synthesis and anti-inflammatory activity of 5-(alkylamino)-N,N-diethyl(1,2,4)triazolo(4,3-a)(1,8)naphthyridine-6-carboxamides with a new substitution pattern on the triazole ring.

机译：1,8-萘啶VI。 5-（烷基氨基）-N，N-二乙基（1,2,4）三唑并（4,3-a）（1,8）萘啶-6-羧酰胺的合成及抗炎活性三唑环。

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On the basis of the good anti-inflammatory properties shown by the 9-alkyl-N,N-dialkyl-5-(alkylamino)[1,2,4]triazolo[4,3-a][1,8]naphthyridine-6-carb oxamides 1, a series of analogues of such compounds, in which the 9-alkyl substituent was replaced by an ester or amide group (compounds 3a-i), was prepared and tested (inhibition of carrageenan-induced paw edema in the rat). Also two 5-(N-alkyl,N-acylamino) derivatives (compounds 4a,b) were synthesized and evaluated for the same purpose. Even though the general trend for these new [1,2,4]triazolo[4,3-a][1,8]naphthyridine derivatives was a decrease in activity compared with compounds 1, some of the new synthesized compounds exhibited still good anti-inflammatory properties.

机译：基于9-烷基-N，N-二烷基-5-（烷基氨基）[1,2,4]三唑并[4,3-a] [1,8]萘啶-显示的良好的抗炎特性。制备并测试了6-碳水化合物草酰胺1（这类化合物的一系列类似物，其中的9-烷基取代基被酯或酰胺基取代）（化合物3a-i）（抑制角叉菜胶诱发的爪水肿）。鼠）。还合成了两种5-（N-烷基，N-酰基氨基）衍生物（化合物4a，b），并出于相同目的对其进行了评估。尽管这些新的[1,2,4]三唑并[4,3-a] [1,8]萘啶衍生物的总体趋势是与化合物1相比活性降低，但一些新合成的化合物仍显示出良好的抗-炎症特性。

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来源
《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2008年第3期|共11页
作者
Di-Braccio M; Grossi G; Roma G; Piras D; Mattioli F; Gosmar M;
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正文语种 eng
中图分类医药、卫生;劳动卫生;
关键词
naphthyridine; Synthesis; Pattern; VI;

机译：萘啶;合成;模式;VI;

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1. 1,8-Naphthyridines VI. Synthesis and anti-inflammatory activity of 5-(alkylamino)-N,N-diethyl(1,2,4)triazolo(4,3-a)(1,8)naphthyridine-6-carboxamides with a new substitution pattern on the triazole ring. [J] . Di-Braccio M, Grossi G, Roma G, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2008,第3期

机译：1,8-萘啶VI。 5-（烷基氨基）-N，N-二乙基（1,2,4）三唑并（4,3-a）（1,8）萘啶-6-羧酰胺的合成及抗炎活性三唑环。
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. Synthesis antimicrobial and anti-inflammatory activity of novel S-substituted and N-substituted 5-(1-adamantyl)-124-triazole-3-thiols [O] . Ebtehal S Al-Abdullah, Hanadi H Asiri, Siham Lahsasni, 2014

机译：新型S-取代和N-取代的5-（1-金刚烷基）-124-三唑-3-硫醇的合成抗菌和抗炎活性
5. Synthesis and Identification of Some New Derivatives of (Benzyl Thio) Benzimidazole -N- (Methylene-5-Yl) - 4,5- Di Substituted 1,2,4-Triazole and Evaluation of Their Activity as Antimicrobial and Anti-Inflammatory Agents [O] . Suaad M. H. Al-Majidi, Halah A.R. Ibrahim, Yasser A.H. AL-issa 2021

机译：（苄基硫代）苯并咪唑-N-（亚甲基-5-基） - 4,5-二甲基取代的1,2,4-三唑的一些新衍生物的合成及鉴定及其作为抗微生物和抗炎的活性评价代理人
6. Synthesis and Biological Activity of Substituted Urea and Thiourea Derivatives Containing 1,2,4-Triazole Moieties. [R] . Kocyigit-Kaymakcioglu, B., Celen, A. O., Tabanca, N., 2013

机译：含1,2,4-三唑部分的取代脲和硫脲衍生物的合成及生物活性。

1,8-Naphthyridines VI. Synthesis and anti-inflammatory activity of 5-(alkylamino)-N,N-diethyl(1,2,4)triazolo(4,3-a)(1,8)naphthyridine-6-carboxamides with a new substitution pattern on the triazole ring.

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