期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 8, 页码 2313-2318出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.02.073
关键词
PTP1B inhibitors; Selectivity; In vivo insulin-sensitising effects
资金
- National Natural Science Foundation of China [20972192]
- Beijing Natural Science Foundation [7102117]
- National S & T Major Project [2012ZX09103-101-063]
- National Institutes of Health [CA152194]
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 mu M 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. (C) 2013 Elsevier Ltd. All rights reserved.
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