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Synthesis of constrained benzocinnolinone analogues of CEP-26401 (irdabisant) as potent, selective histamine H3 receptor inverse agonists.

Abstract：

:A novel class of benzocinnolinones analogs of irdabisant were designed and synthesized as histamine H3R antagonists/inverse agonists. Modifications to the pyridazinone portion of the core and linker led to the identification of molecules with excellent target potency and selectivity with improved rat pharmacokinetic properties and reduced potential hERG liabilities.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Josef KA,Aimone LD,Lyons J,Raddatz R,Hudkins RL

doi

10.1016/j.bmcl.2012.04.001

subject

Has Abstract

pub_date

2012-06-15 00:00:00

pages

4198-202

issue

12

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)00440-4

journal_volume

22

pub_type

杂志文章

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