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Isothiazolidinone inhibitors of PTP1B containing imidazoles and imidazolines |
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| Authors: | Douty Brent Wayland Brian Ala Paul J Bower Michael J Pruitt James Bostrom Lori Wei Min Klabe Ronald Gonneville Lucie Wynn Richard Burn Timothy C Liu Phillip C C Combs Andrew P Yue Eddy W |
| Affiliation: | Incyte Corporation, Discovery Chemistry, Experimental Station, Route 141 and Henry Clay Road, Wilmington, DE 19880, USA. bdouty@incyte.com |
| Abstract: | The structure-based design and synthesis of isothiazolidinone (IZD) inhibitors of PTP1B containing imidazoles and imidazolines and their modification to interact with the B site of PTP1B are described here. The X-ray crystal structures of 3I and 4I complexed with PTP1B were solved and revealed the inhibitors are interacting extensively with the B site of the enzyme. |
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