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

Bioorganic & Medicinal Chemistry Letters
Piyasena HewawasamJ E Starrett

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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Citations

Dec 7, 2007·Naunyn-Schmiedeberg's Archives of Pharmacology·Elfaridah P FrazierMartin C Michel
Apr 20, 2004·Assay and Drug Development Technologies·Ashutosh S PariharChar-Chang Shieh
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Jun 9, 2004·European Journal of Medicinal Chemistry·Giuliana BiagiOreste LeRoy Salerni
Jun 9, 2004·The Journal of Biological Chemistry·Andrea L MeredithRichard W Aldrich
Oct 23, 2019·The Journal of Biological Chemistry·Joseph B O'BrienDavid L Roman
Jul 23, 2019·Clinical and Experimental Pharmacology & Physiology·Jayesh V BeladiyaAnita A Mehta
Jul 28, 2021·Laboratory animal research·Jayesh V Beladiya, Anita A Mehta

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