Medicinal Chemistry

2-(Aryl Oxy Methyl)-1H- Benzimidazoles: Synthesis, Characterization and Biological Evaluation

Abstract

Rekhala John Sunil*, Ramesh Ennam, Sunitha Tharigoppula, Pal Sarbani and Jayashree Ani Reddy

Helminthiasis is a macro, parasitic disease of humans and animals in which a part of the body is infected with Helminth parasites. It is one of the most deadly, neglected, tropical diseases and many die annually from this disease. The total eradication from this problem is very difficult. The drugs which expel Helminth parasites from the body either by stunning or killing them without causing significant damage to the host are called Anthelmintics. The most commonly used class of Anthelmintics are Benzimidazoles, whose mode of action is by blocking transportation of secretory granules and movement of other cell organelles by binding to beta-tubulin and inhibit polymerization of microtubules in the cytoskeleton of the Helminthic parasite. Most of the Anthelmintics are non-selective, with a narrow spectrum of activity, high toxicity, unsafe for undernourished children and pregnant women, requires follow up purgation and development of resistance by the parasite. So there is a need for search and development of new Anthelmintics preferably with a novel mode of action and minimum side effects. Because of this, a scheme was designed which involved synthesis, characterization and Anthelmintic evaluation of some 2-(Aryl Oxy Methyl)-1H-Benzimidazoles. The identification and characterization of the synthesized compounds were carried out by a melting point, thin layer chromatography, FT-IR, 1H-NMR, to ascertain that the synthesized compounds are of different chemical nature than the respective parent compound. The synthesized compounds were preliminarily screened for the in vitro anthelmintic activity using Piperazine Citrate as standard.