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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.

Authors
  • Hewawasam, Piyasena
  • Erway, Matthew
  • Thalody, George
  • Weiner, Harvey
  • Boissard, Christopher G
  • Gribkoff, Valentin K
  • Meanwell, Nicholas A
  • Lodge, Nicholas
  • Starrett, John E Jr
Type
Published Article
Journal
Bioorganic & Medicinal Chemistry Letters
Publisher
Elsevier
Publication Date
Apr 08, 2002
Volume
12
Issue
7
Pages
1117–1120
Identifiers
PMID: 11909730
Source
Medline
License
Unknown

Abstract

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 1,2,4-(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.

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