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Synthesis and characterization of the first inhibitor of N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD).

Beatrice Castellani, Eleonora Diamanti, Daniela Pizzirani, Piero Tardia, Martina Maccesi, Natalia Realini, Paola Magotti, Gianpiero Garau, Thomas Bakkum, Silvia Rivara, Marco Mor, Daniele Piomelli
Chemical Communications : Chem Comm 2017 November 29
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]-1H-quinazoline-6-sulfonamide, ARN19874.

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