Bioorganic & medicinal chemistry

N-Arylated pyrrolidin-2-ones and morpholin-3-ones as potassium channel openers

PH Liang, LW Hsin, CY Cheng

文献索引：Liang, Pi-Hui; Hsin, Ling-Wei; Cheng, Chen-Yu Bioorganic and medicinal chemistry, 2002 , vol. 10, # 10 p. 3267 - 3276

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被引用次数: 30

摘要

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-one (6) and N-(4-benzoylphenyl)-3, 3-dimethyl- pyrrolidin-2-one (9) demonstrated potent and selective relaxant activity at the bladder ...