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Synthesis and characterization of the first inhibitor of N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD)
Chemical Communications ( IF 4.3 ) Pub Date : 2017-11-16 00:00:00 , DOI: 10.1039/c7cc07582k
Beatrice Castellani 1, 2, 3, 4 , Eleonora Diamanti 1, 2, 3, 4 , Daniela Pizzirani 1, 2, 3, 4 , Piero Tardia 1, 2, 3, 4 , Martina Maccesi 4, 5, 6, 7 , Natalia Realini 1, 2, 3, 4 , Paola Magotti 1, 2, 3, 4 , Gianpiero Garau 1, 2, 3, 4 , Thomas Bakkum 1, 2, 3, 4 , Silvia Rivara 4, 8, 9, 10 , Marco Mor 4, 8, 9, 10 , Daniele Piomelli 11, 12, 13, 14
Affiliation  

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.

中文翻译:

N-酰基磷脂酰乙醇胺磷脂酶D(NAPE-PLD)的第一种抑制剂的合成和表征

Ñ -Acylphosphatidylethanolamine磷脂酶d(NAPE-PLD)是一种膜相关的,其催化水解酶锌Ñ -acylphosphatidylethanolamines(NAPEs)转换成脂肪酸乙醇酰胺(的FAE)。在这里,我们描述了第一个小分子NAPE-PLD抑制剂,喹唑啉磺酰胺衍生物2,4-二氧代-N- [4-(4-吡啶基)苯基] -1 H-喹唑啉-6-磺酰胺,ARN19874的鉴定。
更新日期:2017-11-16
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