AI Article Synopsis
- A new group of benzocinnolinones similar to irdabisant was created to act as antagonists/inverse agonists for histamine H3 receptors.
- Adjustments were made to the pyridazinone part and the linker in these compounds, resulting in promising molecules that effectively target their intended receptors.
- These modified compounds showed better effectiveness in rats regarding how they were processed in the body and had lower risks of causing heart-related side effects (hERG liabilities).
Article 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.
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| http://dx.doi.org/10.1016/j.bmcl.2012.04.001 | DOI Listing |
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