501368-40-7Relevant academic research and scientific papers
N-Arylated pyrrolidin-2-ones and morpholin-3-ones as potassium channel openers.
Liang, Pi-Hui,Hsin, Ling-Wei,Cheng, Chen-Yu
, p. 3267 - 3276 (2007/10/03)
Based on the most stable conformation of ZD6169, a series of N-arylated derivatives of oxazolidindione (2), morpholin-3-one (3-5), piperidin-2-one (6), and pyrrolidin-2-one (7-13) was synthesized and evaluated for potassium channel opening activity. In the in-vitro assays, N-(4-benzoylphenyl)-piperidin-2-on (6) and N-(4-benzoylphenyl)-3,3-dimethyl-pyrrolidin-2-one (9) demonstrated potent and selective relaxant activity at the bladder detrusor muscle [IC50, bladder)=7.4 and 6.7 microM, respectively; IC50 ratio (portal vein/bladder)=41 and 51, respectively].
