Bioorganic and Medicinal Chemistry Letters p. 2689 - 2692 (2014)
Update date:2022-07-29
Topics:
Kawasaki, Motoji
Fusano, Akira
Nigo, Tomohiro
Nakamura, Shunya
Ito, Mari N.
Teranishi, Yasuhiro
Matsumoto, Satoshi
Toda, Hiroshi
Nomura, Naruaki
Sumiyoshi, Takaaki
A series of 2,3-disubstituted pyridines were synthesized as potential non-emetic PDE4 inhibitors. 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. Following optimization at the phenoxy group, we identified compound 1 as a potent non-emetic PDE4 inhibitor. Compound 1 showed significant efficacy in an animal model of asthma without inducing emesis.
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