Progress in the development of β-lactams as N-Acylethanolamine Acid Amidase (NAAA) inhibitors: Synthesis and SAR study of new, potent N-O-substituted derivatives

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• 作者：R. Petracca^a ; S. Ponzano^a ; S.M. Bertozzi^a ; O. Sasso^a ; D. Piomelli^a ; ^b ; T. Bandiera^a ; F. Bertozzi^a ; ^{fabio.bertozzi@iit.it}
• 关键词：N-Acylethanolamine acid amidase ; Cysteine hydrolase ; N-O-Substituted β-lactams ; Inhibitors ; Structure&ndash ; activity relationships (SAR)
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：561-575
• 全文大小：1538 K
• 卷排序：126

文摘

SAR exploration on N-O-substituted β-lactams to identify relevant chemical features. Selectivity and physicochemical profile studies on novel N-O-substituted β-lactams. Discovery of N-O-substituted β-lactam 37 with good in vitro and in vivo activity. Characterization of mechanism of action of β-lactam 37 by LC-MS/MS and ABPP.