| Title : Imidazolidine-2,4,5- and pirimidine-2,4,6-triones - New primary pharmacophore for soluble epoxide hydrolase inhibitors with enhanced water solubility - Burmistrov_2020_Bioorg.Med.Chem.Lett_30_126908 |
| Author(s) : Burmistrov V , Morisseau C , D'Yachenko V , Karlov D , Butov GM , Hammock BD |
| Ref : Bioorganic & Medicinal Chemistry Lett , 30 :126908 , 2020 |
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Abstract :
A series of inhibitors of the soluble epoxide hydrolase (sEH) containing imidazolidine-2,4,5-trione or pirimidine-2,4,6-trione has been synthesized. Inhibition potency of the described compounds ranges from 8.4 muM to 0.4 nM. The tested compounds possess higher water solubility than their preceding ureas. Molecular docking indicates new bond between the triones and the active site of sEH that in part explain the observed potency of the new pharmacophores. While less potent than the corresponding ureas, the modifications of urea group reported herein yield compounds with higher water solubility, thus permitting easier formulation. |
| PubMedSearch : Burmistrov_2020_Bioorg.Med.Chem.Lett_30_126908 |
| PubMedID: 31870649 |
Burmistrov V, Morisseau C, D'Yachenko V, Karlov D, Butov GM, Hammock BD (2020)
Imidazolidine-2,4,5- and pirimidine-2,4,6-triones - New primary pharmacophore for soluble epoxide hydrolase inhibitors with enhanced water solubility
Bioorganic & Medicinal Chemistry Lett
30 :126908
Burmistrov V, Morisseau C, D'Yachenko V, Karlov D, Butov GM, Hammock BD (2020)
Bioorganic & Medicinal Chemistry Lett
30 :126908