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In order to search for more potent inhibitors against protein tyrosine phosphatases 1B(PTP1B),which has been verified to be the important therapeutic target for drug design against many kind of diseases including diabetes,obesity1,cancers,etc2.Two series of 2-substituted imino-3-substituted-5-substituted-thiazolidine-4-ones are designed based on analyzing the crystal structure features of the active site of PTP1B3.