N-(5-substituted) thiophene-2-alkylsulfonamides as potent inhibitors of 5-lipoxygenase

被引：37

作者：

Beers, SA

Malloy, EA

Wu, W

Wachter, M

Ansell, J

Singer, M

Steber, M

Barbone, A

Kirchner, T

Ritchie, D

Argentieri, D

机构：

[1] R. W. Johnson Pharmaceutical Res. I., Raritan, NJ 08869

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1997年 / 5卷 / 04期

关键词：

D O I：

10.1016/S0968-0896(97)00025-4

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Compound 4k N-[5-(4-fluoro) phenoxythien-2-yl] methanesulfonamide is representative of a new class of potent inhibitors of 5-lipoxygenase (5-LO). These versatile compounds exhibit dose-dependent inhibition of 5-LO with IC(50)s ranging from 20-100 nM in the rat basophilic leukemia (RBL-1) cell homogenate assay and submicromolar IC,,s in both the RBL-1 and human peripheral blood leukocyte (PBL) whole cell assays. Compound 4k also showed significant anti-inflammatory activity in the adjuvant arthritic rat at an oral dose of 3 mg/kg. (C) 1997 Elsevier Science Ltd.

引用

页码：779 / 786

页数：8

共 9 条

[1]

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