A Potent Cyclooxygenase-2 Inhibitor for Synthesized Pyrimidine and Thiazolopyrimidine Derivatives

被引：5

作者：

Amr, Abd El-Galil E. ^{[1
,2
]}

Al-Omar, Mohamed A. ^{[1
]}

Abdalla, Mohamed M. ^{[3
]}

机构：

[1] King Saud Univ, Coll Pharm, DEDC, Dept Pharmaceut Chem, Riyadh 11451, Saudi Arabia

[2] Natl Res Ctr, Dept Appl Chem, Cairo, Egypt

[3] Saco Pharm Co, Res Unit, 6th October City 11632, Egypt

来源：

INTERNATIONAL JOURNAL OF PHARMACOLOGY | 2016年 / 12卷 / 02期

关键词：

Pyridine derivatives; thiazolopyrimidine; anti-inflammatory activities; COX-2; inhibitors; ANALGESIC ACTIVITY EVALUATION; ANTIINFLAMMATORY ACTIVITY; BIOLOGICAL EVALUATION; ANTICANCER; DESIGN;

D O I：

10.3923/ijp.2016.86.91

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Ten pyridine and pyrimidine and thiazolopyrimidine derivatives (1-10) were synthesized and screened as analgesic, anticonvulsant and antiparkinsonian agent before. Herein, all the target compounds showed anti-inflammatory activity. The active compounds showed selective inhibitory activity towards COX-2 enzyme as revealed by the in vitro enzymatic assay. All the tested compounds proved to have superior gastrointestinal (GI) safety profiles as compared to indomethacin, when tested for their ulcerogenic effects.

引用

页码：86 / 91

页数：6

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