The Discovery and Structure–activity Relationships of 2-(Piperidin-3-yl)-1h-benzimidazoles As Selective, CNS Penetrating H1-antihistamines for Insomnia
Bioorganic & medicinal chemistry letters(2010)
摘要
A series of 2-(3-aminopiperidine)-benzimidazoles were identified as selective H(1)-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 H(1)-antihistamines.
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关键词
H1-Antihistamines,H1-Antagonist,Insomnia, hERG,CNS,Benzimidazole,SAR,Sedative,Selective
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