Deng_2017_Medchemcomm_8_982

Reference

Title : Chiral disubstituted piperidinyl ureas: a class of dual diacylglycerol lipase-alpha and ABHD6 inhibitors - Deng_2017_Medchemcomm_8_982
Author(s) : Deng H , van der Wel T , van den Berg R , van den Nieuwendijk A , Janssen FJ , Baggelaar MP , Overkleeft HS , van der Stelt M
Ref : Medchemcomm , 8 :982 , 2017
Abstract :

Inhibitors of diacylglycerol lipases and alpha,beta-hydrolase domain containing protein 6 (ABHD6) are potential leads for the development of therapeutic agents for metabolic and neurodegenerative disorders. Here, we report the enantioselective synthesis and structure activity relationships of triazole ureas featuring chiral, hydroxylated 2-benzylpiperidines as dual inhibitors of DAGLalpha and ABHD6. The chirality of the carbon bearing the C2 substituent, as well as the position of the hydroxyl (tolerated at C5, but not at C3) has profound influence on the inhibitory activity of both DAGLalpha and ABHD6, as established using biochemical assays and competitive activity-based protein profiling on mouse brain extracts.

PubMedSearch : Deng_2017_Medchemcomm_8_982
PubMedID: 30108813
Gene_locus related to this paper: human-ABHD6

Related information

Inhibitor CHEMBL4289712
Gene_locus human-ABHD6

Citations formats

Deng H, van der Wel T, van den Berg R, van den Nieuwendijk A, Janssen FJ, Baggelaar MP, Overkleeft HS, van der Stelt M (2017)
Chiral disubstituted piperidinyl ureas: a class of dual diacylglycerol lipase-alpha and ABHD6 inhibitors
Medchemcomm 8 :982

Deng H, van der Wel T, van den Berg R, van den Nieuwendijk A, Janssen FJ, Baggelaar MP, Overkleeft HS, van der Stelt M (2017)
Medchemcomm 8 :982