Novel Thioxothiazolo[3,4-a]quinazolin-5(4H)-one Derivatives as BK_Ca Channel Activators for Urinary Incontinence.

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

SUBMITTER: Bae EJ 

PROVIDER: S-EPMC9290006 | biostudies-literature | 2022 Jul

REPOSITORIES: biostudies-literature