Despite the fact that enteroviruses are implicated in a variety of human diseases, there is no approved therapy for the treatment of enteroviral infections. Here, a series of 2,6-dihalophenyl-substituted 1H,3H-thiazolo[3,4-a]benzimidazoles with anti-enterovirus activity is reported. The compounds elicit potent activity against coxsackievirus A9, echovirus 9 and 11 and all six strains of coxsack...

an efficient method has been developed for the catalysis of condensation of 1,2-phenylenediamines and 2-aminothiophenoles with different aldehydes into their corresponding 2-aryl-1h-benzimidazoles and 2-aryl-1h-benzothiazoles under mild condition. in this method, trans-3,5-dihydroperoxy-3,5-dimethyl-1,2-dioxolane (dhpdmdo)/hoac/ki system was used as a novel and effective oxidant in water at roo...

An efficient and green protocol for the synthesis of 2-arylsubstituted benzimidazoles via a condensation reaction of aromatic aldehydes and 1,2-phenylenediamine using nano-Fe3O4@SiO2-SO3H as a solid acid catalyst in ethanol under reflux conditions has been described. The reactions are completed in short times, and the corresponding benzimidaz...

Trisubstituted benzimidazoles have demonstrated potency against Gram-positive and Gram-negative bacterial pathogens. Previously, a library of novel trisubstituted benzimidazoles was constructed for high throughput screening, and compounds were identified that exhibited potency against M. tuberculosis H37Rv and clinical isolates, and were not toxic to Vero cells. A new series of 2-cyclohexyl-5-a...

The antifolate drug methotrexate (MTX) is transported by breast cancer resistance protein (BCRP; ABCG2) and multidrug resistance-associated protein1-4 (MRP1-4; ABCC1-4). In cancer patients, coadministration of benzimidazoles and MTX can result in profound MTX-induced toxicity coinciding with an increase in the serum concentrations of MTX and its main metabolite 7-hydroxymethotrexate. We hypothe...

Pharmaceutically interesting, angular bis-benzimidazoles with three appendages have been synthesized successfully through a diversity-oriented approach with soluble support under microwave irradiation. Polymer immobilized o-phenylenediamine was selectively N-acylated with 2-chloro-3-nitrobenzoic acid in a primary aromatic amino moiety. The obtained amide was cyclized to benzimidazole in an acid...

Benzimidazoles are among the most important nitrogen-containing heterocyclic compounds that have many pharmaceutical applications; including, antitumor, anticancer, anticorrosive, antibacterial, irritant and enzymatic interceptors. In this research, the synthesis of benzimidazoles using o-phenylenediamine and aldehyde derivatives in the presence of the nano montemurillonite in solvent-...

Benzimidazoles are the organic compounds investigated in this work. The experimental determination of the pKa values of protonated benzimidazoles in water is a challenge because of their low solubility. In addition, some derivatives are involved in tautomeric equilibria which increase the complexity of the theoretical pKa determinations. In the present study, different approaches are considered...