Structural highlights
Publication Abstract from PubMed
A novel series of pyrazole sEH inhibitors is reported. Lead optimization efforts to replace the aniline core are also described. In particular, 2-pyridine, 3-pyridine and pyridazine analogs are potent sEH inhibitors with favorable CYP3A4 inhibitory and microsomal stability profiles.
Substituted pyrazoles as novel sEH antagonist: investigation of key binding interactions within the catalytic domain.,Lo HY, Man CC, Fleck RW, Farrow NA, Ingraham RH, Kukulka A, Proudfoot JR, Betageri R, Kirrane T, Patel U, Sharma R, Hoermann MA, Kabcenell A, Lombaert SD Bioorg Med Chem Lett. 2010 Nov 15;20(22):6379-83. Epub 2010 Sep 19. PMID:20934334[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Lo HY, Man CC, Fleck RW, Farrow NA, Ingraham RH, Kukulka A, Proudfoot JR, Betageri R, Kirrane T, Patel U, Sharma R, Hoermann MA, Kabcenell A, Lombaert SD. Substituted pyrazoles as novel sEH antagonist: investigation of key binding interactions within the catalytic domain. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6379-83. Epub 2010 Sep 19. PMID:20934334 doi:10.1016/j.bmcl.2010.09.095
