4,5-diphenyltriazol-3-ones:: Openers of large-conductance Ca2+-activated potassium (maxi-K) channels

被引：32

作者：

Romine, JL

Martin, SW

Gribkoff, VK

Boissard, CG

Dworetzky, SI

Natale, J

Li, Y

Gao, Q

Meanwell, NA

Starrett, JE

机构：

[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Chem, Wallingford, CT 06492 USA

[2] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Neurosci, Wallingford, CT 06492 USA

[3] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Analyt Res & Dev, Wallingford, CT 06492 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2002年 / 45卷 / 14期

关键词：

D O I：

10.1021/jm010569q

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of diphenyl-substituted heterocycles were synthesized and evaluated by electrophysiological techniques as openers of the cloned mammalian large-conductance, Call-activated potassium (maxi-K) channel. The series was designed from deannulation of known benzimidazolone maxi-K opener NS-004 (2) thereby providing an effective template for obtaining structure-activity-related information. The triazolone ring system was the most studied wherein 4,5-diphenyltriazol-3-one 6d (maxi-K = 158%) was identified as the optimal maxi-K channel opener.

引用

页码：2942 / 2952

页数：11

共 34 条

[11]

GRIBKOFF VK, 1996, ADV PHARM SAN DIEGO, V7, P319

[12]

HALLIWELL JV, 1990, K PLUS CHANNELS CENT

[13] NEUROPHARMACOLOGY OF POTASSIUM-ION CHANNELS [J].