Ontology highlight
ABSTRACT:
SUBMITTER: Kiss LE
PROVIDER: S-EPMC6582431 | biostudies-literature | 2018 Oct
REPOSITORIES: biostudies-literature
Kiss László E LE Beliaev Alexandre A Ferreira Humberto S HS Rosa Carla P CP Bonifácio Maria João MJ Loureiro Ana I AI Pires Nuno M NM Palma P Nuno PN Soares-da-Silva Patrício P
ChemMedChem 20180911 20
Fatty acid amide hydrolase (FAAH) can be targeted for the treatment of pain associated with various medical conditions. Herein we report the design and synthesis of a novel series of heterocyclic-N-carboxamide FAAH inhibitors that have a good alignment of potency, metabolic stability and selectivity for FAAH over monoacylglycerol lipase (MAGL) and carboxylesterases (CEs). Lead optimization efforts carried out with benzotriazolyl- and imidazolyl-N-carboxamide series led to the discovery of clinic ...[more]