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Selectivity profiling of novel indene H1-antihistamines for the treatment of insomnia
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Apr2010, Vol. 20 Issue 8, p2629-2633. 5p. - Publication Year :
- 2010
-
Abstract
- Abstract: A series of indene analogs of the H1-antihistamine (−)-R-dimethindene was evaluated for selectivity in the search for potentially improved sedative-hypnotics. Variation of the 6-substitutent in the indene core in combination with a pendant electron rich heterocycle led to the identification of several potent H1-antihistamines with desirable selectivity over CYP enzymes, the M1 muscarinic receptor and the hERG channel. These compounds were candidates for further ADME profiling and in vivo evaluation. [Copyright &y& Elsevier]
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 20
- Issue :
- 8
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 49108826
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.02.055