GIST Scholar
College of Life Sciences and Medical Engineering
Department of Life Sciences
1. Journal Articles
Novel thioxothiazolo[3,4-a]quinazolin-5(4H)-one derivatives as BK(Ca) channel activators for urinary incontinence.
- Type
- Article
- Citation
- ACS Medicinal Chemistry Letters, v.13, no.7, pp.1052 - 1061
- Issued Date
- 2022-06
- Abstract
- Overactive bladder (OAB) is a syndrome causing a sudden and unstoppable need to urinate with significant global prevalence. Several drugs are used to treat OAB; however, they have various side effects. Therefore, new treatment options for OAB are required. A series of novel 5-oxo-N-phenyl-1-thioxo-4,5-dihydro-1H-thiazolo[3,4-a]quinazoline-3-carboxamide derivatives were synthesized and evaluated for their large-conductance voltage-and Ca2+-activated K+ channel activation through a cell-based fluorescence assay and electrophysiological recordings. Several compounds, including a 7-bromo substituent on the heterocyclic system, showed increased channel currents. Among the derivatives, compound 12h exhibited potent in vitro activity with a half-maximal effective concentration (EC50) of 2.89 mu M, good oral pharmacokinetic properties (area under the curve and half-life), and in vivo efficacy in a spontaneously hypertensive rat model.
- Publisher
- Amer Chemical Soc
- ISSN
- 1948-5875
- Appears in Collections:
- Department of Chemistry > 1. Journal Articles
Department of Life Sciences > 1. Journal Articles
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