Optimization of 1,2,5-thiadiazole carbamates as potent and selective ABHD6 inhibitors.

Patel, Jayendra Z; Nevalainen, Tapio J; Savinainen, Juha R; Adams, Yahaya; Laitinen, Tuomo; Runyon, Robert S; Vaara, Miia; Ahenkorah, Stephen; Kaczor, Agnieszka A; Navia-Paldanius, Dina; Gynther, Mikko; Aaltonen, Niina; Joharapurkar, Amit A; Jain, Mukul R; Haka, Abigail S; Maxfield, Frederick R; Laitinen, Jarmo T; Parkkari, Teija

Patel, Jayendra Z; Nevalainen, Tapio J; Savinainen, Juha R; Adams, Yahaya; Laitinen, Tuomo; Runyon, Robert S; Vaara, Miia; Ahenkorah, Stephen; Kaczor, Agnieszka A; Navia-Paldanius, Dina; Gynther, Mikko; Aaltonen, Niina; Joharapurkar, Amit A; Jain, Mukul R; Haka, Abigail S; Maxfield, Frederick R; Laitinen, Jarmo T; Parkkari, Teija.

Affiliation

Patel JZ; School of Pharmacy, University of Eastern Finland, P.O. Box 1627, 70211 Kuopio (Finland). jayendra.patel@uef.fi.

ChemMedChem ; 10(2): 253-65, 2015 Feb.

Article in En | MEDLINE | ID: mdl-25504894

Subject(s)

Carbamates/chemistry; Enzyme Inhibitors/chemistry; Monoacylglycerol Lipases/antagonists & inhibitors; Thiadiazoles/chemistry; Amidohydrolases/antagonists & inhibitors; Amidohydrolases/metabolism; Animals; Binding Sites; Brain/metabolism; Carbamates/chemical synthesis; Carbamates/metabolism; Catalytic Domain; Cell Membrane/metabolism; Enzyme Inhibitors/chemical synthesis; Enzyme Inhibitors/metabolism; HEK293 Cells; Humans; Kinetics; Lipase/antagonists & inhibitors; Lipase/metabolism; Mice; Molecular Docking Simulation; Monoacylglycerol Lipases/genetics; Monoacylglycerol Lipases/metabolism; Protein Binding; Structure-Activity Relationship; Thiadiazoles/chemical synthesis; Thiadiazoles/metabolism

Key words

1,2,5-thiadiazole carbamates; 2-arachidonoylglycerol; ABHD6; cannabinoids; homology modeling; receptors

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Thiadiazoles / Carbamates / Enzyme Inhibitors / Monoacylglycerol Lipases Limits: Animals / Humans Language: En Journal: ChemMedChem Journal subject: FARMACOLOGIA / QUIMICA Year: 2015 Document type: Article Country of publication: Germany

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