1248722-86-2Relevant academic research and scientific papers
The discovery and structure-activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles as selective, CNS penetrating H1-antihistamines for insomnia
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
, p. 2916 - 2919 (2010)
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 compounds. One example, 9q, retained a suitable selectivity profile with CNS exposure equivalent to known centrally active H1-antihistamines.
