New 2-amino- and 2-hydroxymethylbenzimidazoles were synthesized and used to prepare the previously unknown 1,2,3-tri- and 1,2,3,5-tetrasubstituted benzimidazolium bromides with a biphenyl-containing substituent at the imidazole nitrogen atom. In some cases, these bromides exhibit activity against targets associated with diabetes mellitus. These compounds are strong protein tyrosine phosphatase 1B (PTP1B) inhibitors, exhibit chelating and antiglycation activity, but have no significant AT 1 receptor antagonist activity. Hence, biphenyl-containing benzimidazolium derivatives can be considered as a basis for the development of new promising agents for the treatment of type 2 diabetes mellitus (DM2) and other diseases mediated by high phosphatase PTP1B activity.

中文翻译：

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2-氨基和2-羟甲基苯并咪唑溴化物作为蛋白酪氨酸磷酸酶1B（PTP1B）抑制剂和其他与糖尿病相关的靶点

合成了新的 2-氨基和 2-羟甲基苯并咪唑，并用于制备以前未知的 1,2,3-三和 1,2,3,5-四取代苯并咪唑溴化物，在咪唑氮原子处具有含联苯的取代基。在某些情况下，这些溴化物表现出针对与糖尿病相关的靶标的活性。这些化合物是强蛋白酪氨酸磷酸酶 1B (PTP1B) 抑制剂，具有螯合和抗糖化活性，但没有显着的 AT 1 受体拮抗剂活性。因此，含联苯的苯并咪唑鎓衍生物可被视为开发用于治疗 2 型糖尿病 (DM2) 和其他由高磷酸酶 PTP1B 活性介导的疾病的新药物的基础。