A new class of histamine H 3 receptor antagonists derived from ligand based design

Design and synthesis of highly potent and selective non-imidazole inverse agonists for the histamine H 3 receptor is described. The study validates a new pharmacophore model based on the merging of two previously described models. It also demonstrates that the removal of the basic center potentially...

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 17; no. 13; pp. 3670 - 3675
Main Authors Roche, Olivier, Rodríguez Sarmiento, Rosa María
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 01.07.2007
Subjects
De novo design
Histamine H 3 receptor
Pharmacophore model
SAR
Skelgen
Histamine H 3 receptor
Pharmacophore model
Skelgen
SAR
De novo design
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ISSN0960-894X
1464-3405
DOI10.1016/j.bmcl.2007.04.056

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Summary:Design and synthesis of highly potent and selective non-imidazole inverse agonists for the histamine H 3 receptor is described. The study validates a new pharmacophore model based on the merging of two previously described models. It also demonstrates that the removal of the basic center potentially interacting with ASP3.32 and common to both models leads to loss of activity, whereas the replacement of the second basic center by an acceptor retains the potency.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.04.056