Synthesis and Pharmacological Evaluation of 2,4-Dinitroaryldithiocarbamate Derivatives as Novel Monoacylglycerol Lipase Inhibitors

Monoacylglycerol lipase (MAGL) is responsible for signal termination of 2-arachidonoylglycerol (2-AG), an endocannabinoid neurotransmitter endowed with several physiological effects. Previously, we showed that the arylthioamide scaffold represents a privileged template for designing MAGL inhibitors....

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Veröffentlicht in:	Journal of medicinal chemistry 2012-06, Vol.55 (12), p.5774-5783
Hauptverfasser:	Kapanda, Coco N, Masquelier, Julien, Labar, Geoffray, Muccioli, Giulio G, Poupaert, Jacques H, Lambert, Didier M
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Carbamates - chemical synthesis Carbamates - chemistry Carbamates - metabolism Carbamates - pharmacology Cell Line, Tumor Chemistry Techniques, Synthetic Disulfides - chemistry Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - metabolism Enzyme Inhibitors - pharmacology Humans Inhibitory Concentration 50 Mice Monoacylglycerol Lipases - antagonists & inhibitors Monoacylglycerol Lipases - chemistry Monoacylglycerol Lipases - metabolism Piperazines - chemical synthesis Piperazines - chemistry Piperazines - metabolism Piperazines - pharmacology Structure-Activity Relationship Thiourea - analogs & derivatives Thiourea - chemical synthesis Thiourea - chemistry Thiourea - metabolism Thiourea - pharmacology
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