Title : Discovery of 12-Thiazole Abietanes as Selective Inhibitors of the Human Metabolic Serine Hydrolase hABHD16A - Ahonen_2018_ACS.Med.Chem.Lett_9_1269 |
Author(s) : Ahonen TJ , Savinainen JR , Yli-Kauhaluoma J , Kalso E , Laitinen JT , Moreira VM |
Ref : ACS Med Chem Lett , 9 :1269 , 2018 |
Abstract :
Screening of an in-house library of compounds identified 12-thiazole abietanes as a new class of reversible inhibitors of the human metabolic serine hydrolase. Further optimization of the first hit compound lead to the 2-methylthiazole derivative 18, with an IC50 value of 3.4 +/- 0.2 muM and promising selectivity. ABHD16A has been highlighted as a new target for inflammation-mediated pain, although selective inhibitors of hABHD16A (human ABHD16A) have not yet been reported. Our study presents abietane-type diterpenoids as an attractive starting point for the design of selective ABHD16A inhibitors, which will contribute toward understanding the significance of hABHD16A inhibition in vivo. |
PubMedSearch : Ahonen_2018_ACS.Med.Chem.Lett_9_1269 |
PubMedID: 30613338 |
Gene_locus related to this paper: human-ABHD16A |
Inhibitor | Thiazol-abietane-Cpd18 |
Gene_locus | human-ABHD16A |
Ahonen TJ, Savinainen JR, Yli-Kauhaluoma J, Kalso E, Laitinen JT, Moreira VM (2018)
Discovery of 12-Thiazole Abietanes as Selective Inhibitors of the Human Metabolic Serine Hydrolase hABHD16A
ACS Med Chem Lett
9 :1269
Ahonen TJ, Savinainen JR, Yli-Kauhaluoma J, Kalso E, Laitinen JT, Moreira VM (2018)
ACS Med Chem Lett
9 :1269