a water soluble, bronsted acid, 5-sulfosalicylic acid as an efficient organocatalyst was used for the synthesis of physiologically active 2-substituted benzimidazole derivatives from o-phenylenediamine and aromatic aldehydes in ethanol at reflux condition. cost-effectiveness, use of non-hazardous solvents, metal free and commercially available catalyst, single-step, environmentally friendly gre...

RATIONALE Benzimidazoles and its derivatives represent one of the mainly biological active classes of literature. AIM In this present study aimed to synthesize N-mannich bases derivatives compounds bearing of 2-substituted benzimidazole moiety, in order to investigate their possible biological activity. METHOD Benzimidazole compounds were prepared from the condensation reaction between orth...

Irradiation of 1-substituted benzotriazole arylhydrazones 3a-c, 4a,b and 5a,b with a 16 W low pressure mercury arc-lamp (254 nm) for 24 h gave phenanthridin-6-yl-2-phenyldiazines 9a-c, phenanthridin-6(5H)-ones 10a-c, 1-anilinobenzimidazoles 11a-c, 2-aryl-1H-benzimidazoles 12a-c, 1-arylamino-1H-benzimidazol-2-carboxylic acid ethyl esters 14a,b, 1-aryl-1H, 9H-benzo [4,5][1,2,3] triazolo[1,2-a]te...

Simple 1-substituted 5- and 6-isoxazolyl-benzimidazoles have been shown to be potent inhibitors of the BET bromodomains with selectivity over the related bromodomain of CBP. The reported inhibitors were prepared from simple starting materials in two steps followed by separation of the regioisomers or regioselectively in three steps.

Two libraries of substituted benzimidazoles were designed using a 'scaffold-hopping' approach based on reported MDM2-p53 inhibitors. Substituents were chosen following library enumeration and docking into an MDM2 X-ray structure. Benzimidazole libraries were prepared using an efficient solution-phase approach and screened for inhibition of the MDM2-p53 and MDMX-p53 protein-protein interactions....

A water soluble, Bronsted acid, 5-sulfosalicylic acid as an efficient organocatalyst was used for the synthesis of physiologically active 2-substituted benzimidazole derivatives from o-phenylenediamine and aromatic aldehydes in ethanol at reflux condition. Cost-effectiveness, use of non-hazardous solvents, metal free and commercially available catalyst, single-step, environmentally fri...