The synthesis and structure-activity relationships of 4-aryl-3-aminoquinolin-2-ones: A new class of calcium-dependent, large conductance, potassium (maxi-K) channel openers targeted for post-stroke neuroprotection

被引：130

作者：

Hewawasam, P

Fan, WH

Knipe, J

Moon, SL

Boissard, CG

Gribkoff, VK

Starrett, JE

机构：

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

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

[3] Bristol Myers Squibb Pharmaceut Res Inst, Dept Metab & Pharmacokinet, Wallingford, CT 06492 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 13期

关键词：

D O I：

10.1016/S0960-894X(02)00240-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 4-aryl-3-aminoquinoline-2-one derivatives was synthesized and evaluated as activators of the cloned maxi-K channel mSlo (hSlo) expressed in Xenopus laevis oocytes using electrophysiological methods. A brain penetrable activator of maxi-K channels was identified and shown to be significantly active in the MCAO model of stroke. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：1779 / 1783

页数：5

共 36 条

[1] MSLO, A COMPLEX MOUSE GENE ENCODING MAXI CALCIUM-ACTIVATED POTASSIUM CHANNELS [J].