SYNTHESIS OF CARBOXYALKYLTHIOTRIAZOLES AND BICYCLIC DERIVATIVES WITH ANTIINFLAMMATORY AND ANALGESIC ACTIVITY

被引:0
|
作者
MAZZONE, G
PIGNATELLO, R
MAZZONE, S
PANICO, A
BARBERA, F
CATTI, T
CHIECHIO, S
ARRIGOREINA, R
CASTORINA, C
RUSSO, A
机构
[1] IST FARMACOL & FARMACOGNOSIA, I-95125 CATANIA, ITALY
[2] IST CHIM BIOL, I-95125 CATANIA, ITALY
来源
FARMACO | 1992年 / 47卷 / 02期
关键词
D O I
暂无
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
3-Carboxyalkylthio derivatives of 5-alkoxyphenyl-1,2,4-triazole were prepared, performing some substitutions both on carboxyalkyl chain, by lengthening it or introducing substituents with increasing molecular weight in alpha- at the carboxy group, and on N-4 atom in the triazole ring, by introducing an amino or methyl group, so that to vary steric conformation along with the lipophilicity of molecules. The corresponding bicyclic thiazolo-triazolone and triazolo-thiazinone derivatives, which represent the rigid models of carboxymethylthio- and carboxyethylthio- open structures, were also obtained. All the compounds show "in vivo" antiinflammatory activity, while only carboxyalkylthio derivatives of 4-amino- and 4-methyltriazole display an appreciable analgesic one. From the relief of some data on substituent present in the synthesized compounds, a structure-activity relationship is also suggested.
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页码:149 / 169
页数:21
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