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Bicyclic and tricyclic heterocycle derivatives as histamine H3 receptor antagonists for the treatment of obesity.

Authors :
de Lera Ruiz M
Zheng J
Berlin MY
McCormick KD
Aslanian RG
West R
Hwa J
Lachowicz J
van Heek M
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Nov 01; Vol. 23 (21), pp. 6004-9. Date of Electronic Publication: 2013 Aug 19.
Publication Year :
2013

Abstract

A novel series of non-imidazole bicyclic and tricyclic histamine H3 receptor antagonists has been discovered. Compound 17 was identified as a centrally penetrant molecule with high receptor occupancy which demonstrates robust oral activity in rodent models of obesity. In addition compound 17 possesses clean CYP and hERG profiles and shows no behavioral changes in the Irwin test.<br /> (Copyright © 2013 Elsevier Ltd. All rights reserved.)

Details

Language :
English
ISSN :
1464-3405
Volume :
23
Issue :
21
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
24035485
Full Text :
https://doi.org/10.1016/j.bmcl.2013.08.013