SYNTHESIS AND CARBONIC-ANHYDRASE INHIBITORY ACTIVITY OF 4-SUBSTITUTED 2-THIOPHENESULFONAMIDES

被引：20

作者：

HOLMES, JM

LEE, GCM

WIJONO, M

WEINKAM, R

WHEELER, LA

GARST, ME

机构：

[1] ALLERGAN PHARMACEUT INC,DEPT CHEM SCI,IRVINE,CA 92715

[2] ALLERGAN PHARMACEUT INC,DEPT BIOL SCI,IRVINE,CA 92715

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1994年 / 37卷 / 11期

关键词：

D O I：

10.1021/jm00037a015

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 4-substituted 2-thioehenesulfonamides was prepared from 3-thiophenecarboxaldehyde using metalation chemistry developed for 3-furaldehyde. Several of these compounds inhibit carbonic anhydrase II in vitro at concentrations of less than 10 nM. In addition, none of these compounds exhibit sensitization potential as determined from in vitro measurement of cysteine reactivity.

引用

页码：1646 / 1651

页数：6

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