Abstract
Synthesis of a series of novel substituted benzimidazole derivatives by the condensation of o- phenylenediamine (OPDA, 1) with 4-bromobenzoic acid (2) and subsequent reactions of the benzimidazole with different electrophilic reagents is reported. The latter compounds were reacted with styrene and tert-butyl acrylate following Heck Coupling. All the compounds synthesized were screened for their potential anti-bacterial, anti-asthmatic and anti-diabetic properties, which exibibited some promising results towards testing organism in vivo.
Highlights
Benzimidazoles are among the important heterocyclic compounds found in several natural and non-natural products such as Vitamin B121, marine alkaloid kealiiquinone[2], benzimidazole nucleosides[3] etc
We have published some series of biologically active benzimidazoles[9]
The anti-asthmatic activity was carried out using Phosphodiesterase IV enzyme (PDE-IV)[16] (Table 3) and the primary screening of the compounds was done at 1uM concentration using human PDIV enzyme, where Rolipram & Ariflo were used as standard compounds
Summary
Benzimidazoles are among the important heterocyclic compounds found in several natural and non-natural products such as Vitamin B121, marine alkaloid kealiiquinone[2], benzimidazole nucleosides[3] etc. Some of their derivatives are marketed as anti-fungal agents such as Carbendazim[4], anti-helmintic agents such as Mebendazole and thiabendazole[5] and anti-psychotic drug such as Pimozide 6 and other derivatives have been found to possess some interesting bioactivities such as anti-tubercular[7], anti-cancer[8] etc. Owing to the immense biological importance of benzimidazole derivatives, we synthesized some substituted alkenylbenzimidazoles and screened them for biological activity
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