Benzisothiazolinone Derivatives as Potent Allosteric Monoacylglycerol Lipase Inhibitors That Functionally Mimic Sulfenylation of Regulatory Cysteines.

doi:10.1021/acs.jmedchem.9b01679

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Article

Benzisothiazolinone Derivatives as Potent Allosteric Monoacylglycerol Lipase Inhibitors That Functionally Mimic Sulfenylation of Regulatory Cysteines.

Journal of medicinal chemistry - 13 Feb 2020

Castelli Riccardo, Scalvini Laura, Vacondio Federica, Lodola Alessio, Anselmi Mattia, Vezzosi Stefano, Carmi Caterina, Bassi Michele, Ferlenghi Francesca, Rivara Silvia, Møller Ingvar R, Rand Kasper D, Daglian Jennifer, Wei Don, Dotsey Emmanuel Y, Ahmed Faizy, Jung Kwang-Mook, Stella Nephi, Singh Simar, Mor Marco, Piomelli Daniele

Abstract excerpt

We describe a set of benzisothiazolinone (BTZ) derivatives that are potent inhibitors of monoacylglycerol lipase (MGL), the primary degrading enzyme for the endocannabinoid 2-arachidonoyl-sn-glycerol (2-AG). Structure-activity relationship studies evaluated various substitutions on the nitrogen atom and the benzene ring of the BTZ nucleus. Optimized derivatives with nanomolar potency allowed us to investigate the...

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PMID: 31714779
DOI: 10.1021/acs.jmedchem.9b01679

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

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