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Selectivity profiling of novel indene H(1)-antihistamines for the treatment of insomnia.

Abstract：

:A series of indene analogs of the H(1)-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 H(1)-antihistamines with desirable selectivity over CYP enzymes, the M(1) muscarinic receptor and the hERG channel. These compounds were candidates for further ADME profiling and in vivo evaluation.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Li BF,Moree WJ,Yu J,Coon T,Zamani-Kord S,Malany S,Jalali K,Wen J,Wang H,Yang C,Hoare SR,Petroski RE,Madan A,Crowe PD,Beaton G

doi

10.1016/j.bmcl.2010.02.055

subject

Has Abstract

pub_date

2010-04-15 00:00:00

pages

2629-33

issue

8

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00255-6

journal_volume

20

pub_type

杂志文章

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