Microwave-assisted synthesis and pharmacological screening of some triazolothiadiazole derivatives

被引：3

作者：

Gorgu, Ozge ^{[1
]}

Yildirim, Engin ^{[2
]}

Ozkan, Yesim ^{[3
]}

Cakir, Bilge ^{[1
]}

Erol, Kevser ^{[2
]}

Onkol, Tijen ^{[1
]}

机构：

[1] Gazi Univ, Dept Pharmaceut Chem, Fac Pharm, TR-06330 Ankara, Turkey

[2] Osmangazi Univ, Dept Pharmacol, Fac Med, Eskisehir, Turkey

[3] Gazi Univ, Dept Biochem, Fac Pharm, Ankara, Turkey

来源：

BRAZILIAN JOURNAL OF PHARMACEUTICAL SCIENCES | 2020年 / 56卷

关键词：

2(3H)-Benzoxazolone; Triazolothiadiazole; Antinociceptive activity; Microwave-assisted synthesis; BIOLOGICAL EVALUATION; MANNICH-BASES; ACETIC-ACID; DOCKING; 1,2,4-TRIAZOLE; INHIBITORS; DESIGN;

D O I：

10.1590/s2175-97902019000318111

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

In this study, twenty-two new [1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles (5a-n, 6a-h) were synthesized under microwave irradiation (MW1). The chemical structures of the compounds were elucidated by their IR, H-1-NMR, LC-MS, and elemental analysis. The compounds were tested for antinociceptive activity by using the tail clip, tail flick, hot plate, and writhing methods in mice. The varying levels of antinociceptive activity of the compounds were compared with those of aspirin. Among these compounds, compound 5g and 5j were found to be significantly more active than the other compounds and the standard in the tests. Also, inhibitory effects of the test compounds on COX-1 and COX-2 activities were investigated. DuP-697 for COX-2 and SC-560 for COX-1 were used as reference standards.

引用

页数：10

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