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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.

作者信息

Hewawasam Piyasena, Erway Matthew, Thalody George, Weiner Harvey, Boissard Christopher G, Gribkoff Valentin K, Meanwell Nicholas A, Lodge Nicholas, Starrett John E

机构信息

Department of Chemistry, The Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA.

出版信息

Bioorg Med Chem Lett. 2002 Apr 8;12(7):1117-20. doi: 10.1016/s0960-894x(02)00099-9.

DOI:10.1016/s0960-894x(02)00099-9
PMID:11909730
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.

摘要

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