73733-75-2Relevant articles and documents
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
Sharma, Swagat H.,Pablo, Juan Lorenzo,Montesinos, Monica Suarez,Greka, Anna,Hopkins, Corey R.
, p. 155 - 159 (2018/12/11)
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.
New Antihistaminic N-Heterocyclic 4-Piperidinamines. 3. Synthesis and Antihistaminic Activity of N-(4-Piperidinyl)-3H-imidazopyridin-2-amines
Janssens, Frans,Torremans, Joseph,Janssen, Marcel,Stokbroekx, Raymond A.,Luyckx, Marcel,Janssen, Paul A. J.
, p. 1943 - 1947 (2007/10/02)
To study the bioisosteric replacement of a 2-pyridyl ring for a phenyl nucleus in astemizole, a series of N-(4-piperidinyl)-3H-imidazopyridin-2-amines was synthesised and evaluated.The title compounds were obtained starting from either 8a or 8b by four synthetic methods.The in vivo antihistamine activity was evaluated by the compound 48/80-induced lethality test in rats and the histamine-induced lethality test in guinea pigs after oral and/or subcutaneous administration.Compound 37, the isostere of astemizole, showed the most potent antihistaminic properties in the rat.However, astemizole is superior to 37 as to duration of action and total potency.