Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1378939 | Bioorganic & Medicinal Chemistry Letters | 2005 | 5 Pages |
Abstract
A convenient synthetic route to 4-[3-(4-heterocyclylphenylthio)phenyl]-3,4,5,6-tetrahydro-2H-pyran-4-carboxamide analogues as 5-LO inhibitors is described. This methodology enabled rapid development of structure–activity relationships (SARs) leading to improvement of pharmacological properties. Thus, new compounds with higher 5-LO inhibitory potency were discovered. The stereo-chemistry requirements of the tetrahydropyran ring are also discussed.
Graphical abstractThe improved synthesis of 5-LO inhibitor 1 was developed and enabled rapid development of structure–activity relationship.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Takashi Mano, Rodney W. Stevens, Yoshiyuki Okumura, Makoto Kawai, Takako Okumura, Minoru Sakakibara,