Synthesis and characterization of the first inhibitor of N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD). Issue 95 (16th November 2017)

• Record Type: Journal Article
• Authors: Castellani, Beatrice; Diamanti, Eleonora; Pizzirani, Daniela; Tardia, Piero; Maccesi, Martina; Realini, Natalia; Magotti, Paola; Garau, Gianpiero; Bakkum, Thomas; Rivara, Silvia; Mor, Marco; Piomelli, Daniele
• Is Part Of: Chemical communications. Volume 53:Issue 95(2017)
• Page Start: 12814
• Page End: 12817
• Publication Date: 2017-11-16
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/c7cc07582k
• Languages: English
• ISSNs: 1359-7345

Abstract

Abstract : ARN19874 is a quinazolinedione sulfonamide derivative that inhibits NAPE-PLD, a membrane-associated enzyme that cleaves N -acylphosphatidylethanolamines (NAPEs) into fatty acid ethanolamides (FAEs). Abstract : N -Acylphosphatidylethanolamine phospholipase D (NAPE-PLD) is a membrane-associated zinc enzyme that catalyzes the hydrolysis of N -acylphosphatidylethanolamines (NAPEs) into fatty acid ethanolamides (FAEs). Here, we describe the identification of the first small-molecule NAPE-PLD inhibitor, the quinazoline sulfonamide derivative 2, 4-dioxo- N -[4-(4-pyridyl)phenyl]-1 H -quinazoline-6-sulfonamide, ARN19874.