Synthesis and Antinociceptive Activity of Substituted 2-(3-Cyano-4,5,6,7-tetrahydrobenzo[b]thiophene-2-ylamino)-4-oxobut-2-enoates

被引：23
作者：
Gorbunova, I. A. [1 ]
Sharavyeva, Yu. O. [1 ]
Makhmudov, R. R. [1 ]
Shipilovskikh, D. A. [1 ,2 ]
Shadrin, V. M. [3 ]
Pulina, N. A. [3 ]
Shipilovskikh, S. A. [1 ,4 ]
机构：
[1] Perm State Univ, Perm 614990, Russia
[2] Perm Natl Res Polytechn Univ, Perm 614990, Russia
[3] Minist Hlth Russian Federat, Perm State Pharmaceut Acad, Perm 614990, Russia
[4] ITMO Univ, St Petersburg 197101, Russia
来源：
RUSSIAN JOURNAL OF GENERAL CHEMISTRY | 2022年 / 92卷 / 10期
关键词：
Gewald thiophenes; 2; 4-dioxobutane acids; 3-(thiophene-2-yl)imino-3H-furan-2-ones; antinociceptive activity; toxicity; IMINOFURANS; RECYCLIZATION; ANTIMICROBIAL ACTIVITY; ETHYL; DECYCLIZATION; CHEMISTRY; THIENOPYRIMIDINES; ANTIBACTERIAL; DESIGN; ACIDS;
D O I：
10.1134/S1070363222100048
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
A method was proposed for the synthesis of substituted 2-(3-cyano-4,5,6,7-tetrahydrobenzo[b]thiophen-2-ylamino)-4-oxobut-2-enoates containing a nitrile substituent in the thiophene ring by reacting the corresponding 3-thienylimino-3H-furan-2-ones with primary alcohols. The antinociceptive activity and acute toxicity of the obtained compounds were investigated. It was found that the substituted esters have pronounced antinociceptive activity and low toxicity. According to the classification of toxicity of drugs, the obtained substituted of 2-(3-cyano-4,5,6,7-tetrahydrobenzo[b]thiophen-2-ylamino)-4-oxobut-2-enoates belong to the V class toxicity.
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页码：1899 / 1905
页数：7
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