کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1374293 | 981916 | 2010 | 4 صفحه PDF | دانلود رایگان |
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.
A series of 2-(piperidin-3-yl)-1H-benzimidazoles were identified as selective H1-antihistamines for evaluation as potential sedative hypnotics. Representative compounds showed generally 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.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 9, 1 May 2010, Pages 2916–2919