An efficient soluble polymer-supported method has been developed for the parallel synthesis of substituted benzimidazole linked benzoxazoles using focused microwave irradiation. The key step involves the amidation of 4-hydroxy-3-nitrobenzoic acid with polymer-immobilized o-phenylenediamine. Application of mild acidic conditions promoted the ring closure to furnish the benzimidazole ring. After ...

The structure activity relationships of 1H-benzimidazole-8-carboxylic acids (9a-9f), 1H-benzimidazole-8carboxylates (8a-8f) are described. Characteristic compounds showed improved demanding activity over a previously recognized 2-aminobenzimidazole series. In the lead optimization process and structure–activity relationship (SAR) of separate inhibitors based on modification of the lead molecule...

The solution conformations of 2-substituted derivatives of 1-(beta-D-ribofuranosyl)benzimidazole have been determined by circular dichroism spectroscopy in aqueous solutions. It is shown that analogs with methyl, amino, or methylamino substituents at position 2 of the benzimidazole ring (position 8 of the purine ring) have predominantly anti conformations, whereas analogs with chloro, aza, meth...

A large group of benzimidazole derivatives are highly effective as an anthelmintics [ 11. Among these, mebendazole (la, methyl 5-benzoylbenzimidazole-2-carbamate) and flubendazole (lb, methyl 5-p-fluorobenzoylbenzimidazole-Z-carbamate) have demonstrated a broad-spectrum of activity against helminth diseases including filarial infections [2-51. In our continuing studies to develop new antifilari...

A series of novel substituted benzimidazole (7a - n) derivatives were synthesized and characterized by 1H, 13C Nuclear Magnetic Resonance (NMR) spectra High Resolution Mass Spectrometry (HRMS). The substitution was done in position -1 -2 appropriate groups. These compounds are obtained N-alkylation reaction with thiomethyl-1H-benzimidazole intermediates (5a g). Design g) made condensation betwe...

This research includes synthesis of new derivatives benzimidazole , the compound (A1*) prepared by reaction o-phenylene diamine with carbon disulfide in alcoholic potassium hydroxide. Then was ethyl chloroacetate and hydroxide to give ester (A2*). preparation hydrazide (A3*) (A2*) hydrazine hydrate (80%). we used prepare pyrazole (A4), then mannich basses (A4) different primary aromatic amines ...

Objective: The aim of the present work was to synthesize and characterize a series of 6substituted benzimidazole-2-carbamic acid derivatives and evaluate them for antimicrobial activity. Methods: A novel series of 6-substituted benzimidazole-2-carbamic acid derivatives (6a-f) were synthesized by reacting substituted benzyl chlorides (2a-c) with 4-hydroxy -2nitro aniline (3) in the presence of a...