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

doi:10.1039/C7CC07582K

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

Beatrice Castellani,

‡^a Eleonora Diamanti,

‡§^a Daniela Pizzirani,

¶^a Piero Tardia,

^a Martina Maccesi,

^b Natalia Realini,

^a Paola Magotti,

||^a Gianpiero Garau,

**^a Thomas Bakkum,

††^a Silvia Rivara,

^d Marco Mor

^d and Daniele Piomelli

*^c

Author affiliations

* Corresponding authors

^a Drug Discovery and Development, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy

^b Department of Chemistry and Pharmaceutical Sciences, University of Ferrara, Via Fossato Mortara 46, 44121 Ferrara, Italy

^c Departments of Anatomy and Neurobiology, Biochemistry and Pharmacology University of California, Irvine, California, USA
E-mail: piomelli@uci.edu

^d Food and Drug Department, University of Parma, Area delle Scienze 27/A, 43124 Parma, Italy

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]-1H-quinazoline-6-sulfonamide, ARN19874.

Chemical Communications

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

Abstract

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

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