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

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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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