Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10595944 | Bioorganic & Medicinal Chemistry Letters | 2013 | 6 Pages |
Abstract
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 inhibitor of PTP1B. Furthermore, compound 16 demonstrated excellent selectivity to PTP1B over other PTPs. It also displayed in vivo insulin sensitizing effect in the insulin resistant mice.
Keywords
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Yan-Bo Tang, Dianyun Lu, Zheng Chen, Chun Hu, Ying Yang, Jin-Ying Tian, Fei Ye, Li Wu, Zhong-Yin Zhang, Zhiyan Xiao,