• SyncroPatch 384/768i

    世界最速のオートパッチ
  • SyncroPatch 384/768i

    384ch同時測定 => 768chへアップグレード可能
  • SyncroPatch 384/768i

    ギガシールによるHTS
  • SyncroPatch 384/768i

    Analysis Software even more powerful than before
  • SyncroPatch 384/768i

    最先端技術によるアッセイ柔軟性

2019 - Design, synthesis and characterization of novel N-heterocyclic-1-benzyl-1H-benzo[d]imidazole-2-amines as selective TRPC5 inhibitors leading to the identification of the selective compound, AC1903

icon sp96   SyncroPatch 384PE article in Bioorganic and Medicinal Chemistry Letters (2019)

Authors:
Sharma, S.H., Pablo J.L., Montesinos, M.S., Greka, A., Hopkins, C.R.

Journal:
Bioorganic and Medicinal Chemistry Letters (2019) 29(2): 155-159


Abstract:

The transient receptor potential cation channel 5 (TRPC5) has been previously shown to affect podocyte survival in the kidney. As such, inhibitors of TRPC5 are interesting candidates for the treatment of chronic kidney disease (CKD). Herein, we report the synthesis and biological characterization of a series of N-heterocyclic-1-benzyl-1H-benzo[d]imidazole-2-amines as selective TRPC5 inhibitors. Work reported here evaluates the benzimidazole scaffold and substituents resulting in the discovery of AC1903, a TRPC5 inhibitor that is active in multiple animal models of CKD.


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