DuP-983(DuP-983) - 药物靶点：POR_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

POR

作用机制

POR inhibitors(Cytochrome P450 reductase inhibitors)

治疗领域

免疫系统疾病皮肤和肌肉骨骼疾病

在研适应症-

非在研适应症

银屑病

原研机构

Bristol Myers Squibb Co.

在研机构-

非在研机构

Bristol Myers Squibb Co.

最高研发阶段终止临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C22H18FN3O

InChIKeyDZGMNXWTQWGZTK-UHFFFAOYSA-N

CAS号137103-53-8

关联

100 项与 DuP-983 相关的临床结果

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100 项与 DuP-983 相关的转化医学

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100 项与 DuP-983 相关的专利（医药）

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1

项与 DuP-983 相关的文献（医药）

1992-08-01·Journal of Medicinal Chemistry1区 · 医学

Novel 1-(pyridylphenyl)-1-phenyl-2-imidazolylethanols with topical antiinflammatory activity

1区 · 医学

Article

作者: Collins, Robert J. ; Wright, Stephen W. ; Batt, Douglas G. ; Wadman, Eric A. ; Green, Alicia M. ; Harris, Richard R. ; Corbett, Ronald L.

The synthesis, biological evaluation, and structure-activity relationships of a series of 1-(pyridylphenyl)-1-phenyl-2-imidazolylethanols are described. These compounds show potent dose-dependent topical antiinflammatory activity in murine models of skin inflammation. This effect is likely due to inhibition of cytochrome P450 and consequent reduction in levels of 12R-HETE in the skin. These compounds were examined for their ability to inhibit the oxidative metabolism of arachidonic acid; they specifically inhibit the formation of prostacyclins in mouse macrophages. To study the effects of structure on the in vivo activity, three general features of the molecules were varied: the position of attachment of the pyridine nucleus (A), the second aromatic residue (B), and the nitrogen base on the ethanol chain (C). 1-[4-(4-Pyridyl)phenyl]-1-(4-fluorophenyl)-2- imidazolylethanol (2a, DuP 983) shows a very attractive profile of antiinflammatory activity and has been selected for clinical evaluation as a topical antiinflammatory agent.

100 项与 DuP-983 相关的药物交易

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