The discovery and structure–activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles as selective, CNS penetrating H 1-antihistamines for insomnia

…, S Zamani-Kord, WJ Moree, RE Petroski, J Wen…

文献索引：Lavrador-Erb, Karine; Ravula, Satheesh Babu; Yu, Jinghua; Zamani-Kord, Said; Moree, Wilna J.; Petroski, Robert E.; Wen, Jianyun; Malany, Siobhan; Hoare, Samuel R.J.; Madan, Ajay; Crowe, Paul D.; Beaton, Graham Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 9 p. 2916 - 2919

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被引用次数: 11

摘要

A series of 2-(3-aminopiperidine)-benzimidazoles were identified as selective H1- antihistamines for evaluation as potential sedative hypnotics. Representative compounds showed improved hERG selectivity over a previously identified 2-aminobenzimidazole series. While hERG activity could be modulated via manipulation of the benzimidazole N1 substituent, this approach led to a reduction in CNS exposure for the more selective ...