Title : Identification of 2,3-disubstituted pyridines as potent, non-emetic PDE4 inhibitors.

Pub. Date : 2014 Jun 15

PMID : 24794103






2 Functional Relationships(s)
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1 To decrease brain exposure and minimize emesis, we modified the lipophilic moiety of a series of emetic PDE4 inhibitors and found that introduction of a hydroxy group into the pyridine moiety of the side chain led to non-emetic compounds with preserved PDE4 inhibitory activity. pyridine phosphodiesterase 4A Homo sapiens
2 To decrease brain exposure and minimize emesis, we modified the lipophilic moiety of a series of emetic PDE4 inhibitors and found that introduction of a hydroxy group into the pyridine moiety of the side chain led to non-emetic compounds with preserved PDE4 inhibitory activity. pyridine phosphodiesterase 4A Homo sapiens