Synthesis of new thiazolo[ 3,2-b][1,2,4]triazole-6(5H)-one derivatives as potent analgesic and anti-inflammatory agents

被引：23

作者：

Assarzadeh, Mohammad Javad ^{[1
]}

Almasirad, Ali ^{[1
]}

Shafiee, Abbas ^{[2
,3
]}

Koopaei, Mansur Nassiri ^{[1
]}

Abdollahi, Mohammad ^{[3
,4
]}

机构：

[1] Islamic Azad Univ, Pharmaceut Sci Branch, Dept Med Chem, Tehran 19419, Iran

[2] Univ Tehran Med Sci, Fac Pharm, Dept Med Chem, Tehran 14174, Iran

[3] Univ Tehran Med Sci, Pharmaceut Sci Res Ctr, Tehran 14174, Iran

[4] Univ Tehran Med Sci, Fac Pharm, Dept Pharmacol & Toxicol, Tehran 14174, Iran

来源：

MEDICINAL CHEMISTRY RESEARCH | 2014年 / 23卷 / 02期

基金：

美国国家科学基金会;

关键词：

Analgesic agents; Anti-inflammatory activity; Thiazolo-triazole; Ulcerogenic activity; ACID HYDRAZIDES; IBUPROFEN; DESIGN;

D O I：

10.1007/s00044-013-0697-y

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of thiazolo[3,2-b][1,2,4] triazole-6(5H)-ones were synthesized and evaluated for their analgesic and anti-inflammatory activities. The structures of these compounds were supported by FT-IR, (HNMR)-H-1, and Mass spectra. All of the final compounds showed potent analgesic activity and the best compound 9d was 2.4 times more potent than mefenamic acid as the reference drug. In addition, most of them showed comparable or better anti-inflammatory activity in comparison with mefenamic acid and indomethacin. Moreover, compounds 9d, 9e, 9g, 9h, 9i, 9k, 9n, and 9o did not exhibit any significant ulcerogenic activity.

引用

页码：948 / 957

页数：10

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