| Title : Design and synthesis of substituted nicotinamides as inhibitors of soluble epoxide hydrolase - Taylor_2009_Bioorg.Med.Chem.Lett_19_5864 |
| Author(s) : Taylor SJ , Soleymanzadeh F , Eldrup AB , Farrow NA , Muegge I , Kukulka A , Kabcenell AK , De Lombaert S |
| Ref : Bioorganic & Medicinal Chemistry Lett , 19 :5864 , 2009 |
|
Abstract :
A series of potent nicotinamide inhibitors of soluble epoxides hydrolase (sEH) is disclosed. This series was designed using structure-based deconstruction and a combination of two HTS hit series, resulting in hybrid analogs that retained the optimal potency from one series, and acceptable in vitro metabolic stability from the other. Structure-guided optimization of these analogs gave rise to nanomolar inhibitors of human sEH that had acceptable plasma exposure to qualify them as probes to determine the in vivo phenotypic consequences of sEH inhibition. |
| PubMedSearch : Taylor_2009_Bioorg.Med.Chem.Lett_19_5864 |
| PubMedID: 19758802 |
| Inhibitor | 33N |
Taylor SJ, Soleymanzadeh F, Eldrup AB, Farrow NA, Muegge I, Kukulka A, Kabcenell AK, De Lombaert S (2009)
Design and synthesis of substituted nicotinamides as inhibitors of soluble epoxide hydrolase
Bioorganic & Medicinal Chemistry Lett
19 :5864
Taylor SJ, Soleymanzadeh F, Eldrup AB, Farrow NA, Muegge I, Kukulka A, Kabcenell AK, De Lombaert S (2009)
Bioorganic & Medicinal Chemistry Lett
19 :5864