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Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors |
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| Authors: | Zhao Hongyu Liu Gang Xin Zhili Serby Michael D Pei Zhonghua Szczepankiewicz Bruce G Hajduk Philip J Abad-Zapatero Cele Hutchins Charles W Lubben Thomas H Ballaron Stephen J Haasch Deanna L Kaszubska Wiweka Rondinone Cristina M Trevillyan James M Jirousek Michael R |
| Affiliation: | Metabolic Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064-6098, USA. hongyu.zhao@abbott.com |
| Abstract: | Guided by X-ray crystallography, we have extended the structure-activity relationship (SAR) study on an isoxazole carboxylic acid-based PTP1B inhibitor (1) and more potent and equally selective (>20-fold selectivity over the highly homologous T-cell PTPase, TCPTP) PTP1B inhibitors were identified. Inhibitor 7 demonstrated good cellular activity against PTP1B in COS 7 cells. |
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