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Bioorg Med Chem Lett. 2008 Jan 1;18(1):66-71. Epub 2007 Nov 9.

Isothiazolidinone inhibitors of PTP1B containing imidazoles and imidazolines.

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  • 1Incyte Corporation, Discovery Chemistry, Experimental Station, Route 141 and Henry Clay Road, Wilmington, DE 19880, USA.


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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