Patel, Jayendra Z. published the artcileOptimization of 1,2,5-Thiadiazole Carbamates as Potent and Selective ABHD6 Inhibitors, Product Details of C6H9N3O2S, the publication is ChemMedChem (2015), 10(2), 253-265, database is CAplus and MEDLINE.
At present, inhibitors of α/β-hydrolase domain 6 (ABHD6) are viewed as a promising approach to treat inflammation and metabolic disorders. This article describes the development of 1,2,5-thiadiazole carbamates as ABHD6 inhibitors. Altogether, 34 compounds were synthesized, and their inhibitory activity was tested using lysates of HEK293 cells transiently expressing human ABHD6 (hABHD6). Among the compound series, 4-morpholino-1,2,5-thiadiazol-3-yl cyclooctyl(methyl)carbamate I (JZP-430) potently and irreversibly inhibited hABHD6 (IC50=44 nM) and showed ∼230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL), the main off-targets of related compounds Addnl., activity-based protein profiling indicated that I displays good selectivity among the serine hydrolases of the mouse brain membrane proteome. I has been identified as a highly selective, irreversible inhibitor of hABHD6, which may provide a novel approach in the treatment of obesity and type II diabetes.
ChemMedChem published new progress about 30165-97-0. 30165-97-0 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Thiadiazole,Alcohol, name is 4-Morpholino-1,2,5-thiadiazol-3-ol, and the molecular formula is C6H9N3O2S, Product Details of C6H9N3O2S.
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