851888-38-5

Upstream product

• 60639-52-3 N²-methylbenzene-1,2,3-triamine 
• 5910-19-0 N-methyl-2,6-dinitroaniline 
• 106-39-8 bromochlorobenzene 
• 851886-92-5 7-amino-1-methyl-1,3-dihydro-2H-benzimidazol-2-one 

Downstream Products

• 851888-39-6 4-[(4-chlorophenyl)amino]-1-(4-methoxybenzyl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one 
• 851888-40-9 4-[(4-chlorophenyl)(1-methylethyl)amino]-1-(4-methoxybenzyl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one 
• 851888-57-8 N-(4-chlorophenyl)-N-[1-(4-methoxybenzyl)-3-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-4-yl]acetamide 
• 851888-41-0 7-[(4-chlorophenyl)(1-methylethyl)amino]-1-methyl-1,3-dihydro-2H-benzimidazol-2-one 
• 851888-42-1 2-chloro-N-(4-chlorophenyl)-1-methyl-N-(1-methylethyl)-1H-benzimidazol-7-amine 

Relevant academic research and scientific papers

Discovery of a 7-arylaminobenzimidazole series as novel CRF1receptor antagonists

A promising lead compound 1 of a benzimidazole series has been identified as a corticotropin-releasing factor 1 (CRF1) receptor antagonist. In this study, we focused on replacement of a 7-alkylamino group of 1, predicted to occupy a large lipophilic pocket of a CRF1receptor, with an aryl group. During the course of this examination, we established new synthetic approaches to 2,7-diarylaminobenzimidazoles. The novel synthesis of 7-arylaminobenzimidazoles culminated in the identification of compounds exhibiting inhibitory activities comparable to the alkyl analog 1. A representative compound, p-methoxyanilino analog 16g, showed potent CRF binding inhibitory activity against a human CRF1receptor and human CRF1receptor antagonistic activity (IC50?=?27?nM, 56?nM, respectively). This compound exhibited ex vivo125I-Tyr0(125I-CRF) binding inhibitory activity in mouse frontal cortex, olfactory bulb, and pituitary gland at 20?mg/kg after oral administration. In this report, we discuss the structure–activity-relationship of these 7-arylamino-1H-benzimidazoles and their synthetic method.