1H-2,3-二氢嘧啶衍生物：一类新型有效的蛋白酪氨酸磷酸酶 1B 抑制剂。
1H-2,3-dihydroperimidine derivatives: a new class of potent protein tyrosine phosphatase 1B inhibitors.
机构信息
School of Pharmaceutical Science, Jiangnan University, Wuxi 214122, China.
出版信息
Molecules. 2013 Dec 23;19(1):102-21. doi: 10.3390/molecules19010102.
A series of 1H-2,3-dihydroperimidine derivatives was designed, synthesized, and evaluated as a new class of inhibitors of protein tyrosine phosphatase 1B (PTP1B) with IC50 values in the micromolar range. Compounds 46 and 49 showed submicromolar inhibitory activity against PTP1B, and good selectivity (3.48-fold and 2.10-fold respectively) over T-cell protein tyrosine phosphatases (TCPTP). These results have provided novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs.
设计、合成了一系列 1H-2,3-二氢嘧啶并[4,5-d]嘧啶衍生物，并将其作为新型蛋白酪氨酸磷酸酶 1B（PTP1B）抑制剂进行了评价，其半数抑制浓度（IC50）在微摩尔范围内。化合物 46 和 49 对 PTP1B 表现出亚微摩尔抑制活性，对 T 细胞蛋白酪氨酸磷酸酶（TCPTP）具有良好的选择性（分别为 3.48 倍和 2.10 倍）。这些结果为设计 PTP1B 及其他 PTP 的抑制剂提供了新的先导化合物。
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