B. Shivakumar

Benzimidazole is the heterocyclic compound which contains a phenyl ring fused to an imidazole ring, Benzimidazole analogs are of crucial importance because of their different clinical applications and biological activity. Benzimidazoles are known as an optimistic class of bioactive heterocyclic compounds possessing a wide variety of biological activities. Benzimidazole derivatives play an important role in medical field with so many pharmacological activities such as antimicrobial, antiviral, anticancer activity, antioxidant, antiparasitic, antiproliferative, antitumor, anti-HIV, anticonvulsant, antiprotozoal, analgesic and anti-inflammatory, antihypertensive, anticancer, androgen receptor antagonist, vasorelaxant etc. This review is summarized to understand the chemistry of various derivatives of substituted benzimidazoles with their pharmacological activities.

A new series of 4-(2-chloroquinolin-3-yl)-6-(6-methyl-1H-benzimidazol-2-yl)pyrimidin-2-amine (Va-k) have been synthesized by the reaction of 3-(2-chloroquinolin-3-yl)-1-(6-methyl-1H-benzimidazol-2-yl)prop-2-en-1-one (IVa-k) with guanidine nitrate in ethanol and aqueous solution of sodium hydroxide. The synthesized compounds were characterized by their IR, 1H NMR and Mass spectral studies. The synthesized compounds were evaluated for anthelmintic activity by in-vitro method, against south Indian adult earth worms Pheretima posthuma using Albendazole as a standard drug. Results of the activities reveal that, compounds exhibited moderate to good anthelmintic activity.

The aceclofenac sodium loaded calcium alginate (CA) based microbeads prepared by ionotropic external gelation technique with calcium chloride as cross-linking agent. Calcium alginate microbeads represent a useful tool for oral sustained/ controlled drug delivery but show several problems, mainly related to the stability, and rapid drug release at higher pH that, in most cases, is too fast due to increase porosity. To overcome such inconveniences, which was to develop CA microbeads coated with xyloglucan (XG) as drug release modifier to improve stability and prolong the drug release. The mean particle sizes of drug-loaded microbeads were found to be in the range 476.45±12 to 765.10 ± 0.22. The drug entrapment efficiency was obtained in the range of 62.24±0.66 to 102.75 ± 0.87.The shape and surface characteristics were determined by scanning electron microscopy (SEM). No significant drug-polymer interactions, physical changes and crystallinity of the drug in the formulations were determined by FT-IR spectroscopy, differential scanning calorimetry (DSC) and X-ray powder diffraction [XPRD]. In-vitro drug release profiles of microbeads were pH dependent and were analyzed by different kinetic models. The mechanism of drug release from microbeads depends on swelling and erosion process resulting CA microbeads was diffusion controlled followed by First order kinetics and whereas CA microbeads coated with XG approaching to near Zero- order kinetics.