STYRYLPYRAZOLES, STYRYLISOXAZOLES, AND STYRYLISOTHIAZOLES - NOVEL 5-LIPOXYGENASE AND CYCLOOXYGENASE INHIBITORS

被引：106

作者：

FLYNN, DL

BELLIOTTI, TR

BOCTOR, AM

CONNOR, DT

KOSTLAN, CR

NIES, DE

ORTWINE, DF

SCHRIER, DJ

SIRCAR, JC

机构：

[1] WARNER LAMBERT PARKE DAVIS,DIV PHARMACEUT RES,DEPT CHEM,ANN ARBOR,MI 48105

[2] WARNER LAMBERT PARKE DAVIS,DIV PHARMACEUT RES,DEPT PHARMACOL,ANN ARBOR,MI 48105

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1991年 / 34卷 / 02期

关键词：

D O I：

10.1021/jm00106a006

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles were prepared and found to be dual inhibitors of 5-lipoxygenase and cyclooxygenase in rat basophilic leukemia cells. Compounds from this series also were found to inhibit the in vivo production of LTB4 when dosed orally in rats. Among these compounds, di-tert-butylphenols 19 and 33 exhibit oral activity in various models of inflammation and, most importantly, are devoid of ulcerogenic potential.

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页码：518 / 525

页数：8

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