Design, synthesis and insulin-sensitising effects of novel PTP1B inhibitors

YB Tang, D Lu, Z Chen, C Hu, Y Yang, JY Tian…

文献索引：Tang, Yan-Bo; Lu, Dianyun; Chen, Zheng; Hu, Chun; Yang, Ying; Tian, Jin-Ying; Ye, Fei; Wu, Li; Zhang, Zhong-Yin; Xiao, Zhiyan Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 8 p. 2313 - 2318

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被引用次数: 9

摘要

Fifteen novel sulfathiazole-related compounds were designed as PTP1B inhibitors based on a previously reported allosteric inhibitor (1) of PTP1B. These compounds were synthesized and evaluated against human recombinant PTP1B. Six compounds (3, 4, 8 and 14–16) exhibited significant inhibitory activity against PTP1B. The most active compound (16) showed IC50 value of 3.2 μM and kinetic analysis indicated that it is a non-competitive ...