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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

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

Swagat H Sharma, Juan Lorenzo Pablo, Monica Suarez Montesinos, Anna Greka, Corey R Hopkins

Bioorg Med Chem Lett. 2019 Jan 15;29(2):155-159.

PMID: 30538066

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP831234130	AC1903		831234-13-0	Price

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