Synthesis and characterization of the first inhibitor of<i>N</i>-acylphosphatidylethanolamine phospholipase D (NAPE-PLD)
作者: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
日期:——
(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.
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。