The synthesis and structure-activity relationships of 1,3-diaryl 1,2,4-(4H)-triazol-5-ones:: A new class of calcium-dependent, large conductance, potassium (Maxi-K) channel opener targeted for urge urinary incontinence

被引：31

作者：

Hewawasam, P

Erway, M

Thalody, G

Weiner, H

Boissard, CG

Gribkoff, VK

Meanwell, NA

Lodge, N

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 Genitourinary Drug Discovery, Wallingford, CT 06492 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(02)00099-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 1,3-diaryl 1,2,4-(4H)-triazol-5-ones was prepared and shown by electrophysiological analysis to activate a cloned maxi-K channel mSlo (or hSlo) expressed in Xenopus laevis oocytes. The effects of these structurally novel maxi-K channel openers on bladder contractile function were studied in vitro using isolated rat bladder strips pre-contracted with carbachol. Several 1,3-diaryl l,2,4-(4H)-triazol-5-one derivatives were found to be potent smooth muscle relaxants but this activity did not completely correlate with maxi-K channel opening. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：1117 / 1120

页数：4

共 20 条

[1]

ABRAMS P, 1988, SCAND J UROL NEPHROL, P5

[2]

*AHCPR, 1996, AHCPR PUBL

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