Discovery of 4-[(5-arylidene-4-oxothiazolidin-3-yl)methyl]benzoic acid derivatives active as novel potent allosteric inhibitors of protein tyrosine phosphatase 1B: In silico studies and in vitro evaluation as insulinomimetic and anti-inflammatory agents

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• 作者：Rosaria Ottanà ; ^a ; Paolo Paoli^b ; Alexandra Naß ; ^c ; Giulia Lori^b ; Venera Cardile^d ; Ilenia Adornato^a ; Archimede Rotondo^e ; Adriana Carol Eleonora Graziano^d ; Gerhard Wolber^c ; Rosanna Maccari^a ; ^{rmaccari@unime.it}
• 关键词：Protein tyrosine phosphatases ; Enzyme inhibitors ; Insulinomimetic effects ; Anti-inflammatory activity ; Molecular docking ; 5-Arylidene-4-thiazolidinone derivatives
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：840-858
• 全文大小：2930 K
• 卷排序：127

文摘

Insulin resistance and inflammation are implicated in diabetes mellitus and obesity. Protein tyrosine phosphatase 1B (PTP1B) inhibitors act as insulin-sensitizing agents. New 4-thiazolidinone derivatives were found to be potent PTP1B inhibitors. Several tested compounds exhibited insulinomimetic and/or anti-inflammatory activity. A new lead compound endowed with a promising cellular activity profile was identified.