Towards multi-target antidiabetic agents: Discovery of biphenyl-benzimidazole conjugates as AMPK activators.

Denis A Babkov, Olga N Zhukowskaya,Alexander V Borisov, Valentina A Babkova, Elena V Sokolova,Anastasia A Brigadirova,Roman A Litvinov,Alexandra A Kolodina,Anatolii S Morkovnik,Vadim S Sochnev,Gennady S Borodkin,Alexander A Spasov

Bioorganic & Medicinal Chemistry Letters（2019）

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摘要

•New biphenyl derivatives of tricyclic benzimidazoles were synthesized.•2′-Cyanobiphenyl was identified as novel pharmacophore of AMPK-activating activity.•Lead compounds demonstrate submicromolar potency towards AMPK.•One of lead compounds target AMPK and AT1 receptor simultaneously.•One of derivatives is a potent inhibitor of advanced protein glycation end-products.

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关键词

Fused benzimidazoles,Biphenyl,Antidiabetic activity,AMP-activated protein kinase

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