The therapeutic journey of benzimidazoles: A review

Molecular Modelling Lab (MML), Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, Punjab 147002, India.
Bioorganic & medicinal chemistry (Impact Factor: 2.79). 09/2012; 20(21):6208-36. DOI: 10.1016/j.bmc.2012.09.013
Source: PubMed


Presence of benzimidazole nucleus in numerous categories of therapeutic agents such as antimicrobials, antivirals, antiparasites, anticancer, anti-inflammatory, antioxidants, proton pump inhibitors, antihypertensives, anticoagulants, immunomodulators, hormone modulators, CNS stimulants as well as depressants, lipid level modulators, antidiabetics, etc. has made it an indispensable anchor for development of new therapeutic agents. Varied substitutents around the benzimidazole nucleus have provided a wide spectrum of biological activities. Importance of this nucleus in some activities like, Angiotensin I (AT(1)) receptor antagonism and proton-pump inhibition is reviewed separately in literature. Even some very short reviews on biological importance of this nucleus are also known in literature. However, owing to fast development of new drugs possessing benzimidazole nucleus many research reports are generated in short span of time. So, there is a need to couple the latest information with the earlier information to understand the current status of benzimidazole nucleus in medicinal chemistry research. In the present review, various derivatives of benzimidazole with different pharmacological activities are described on the basis of substitution pattern around the nucleus with an aim to help medicinal chemists for developing an SAR on benzimidazole derived compounds for each activity. This discussion will further help in the development of novel benzimidazole compounds.

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    • "Antimicrobial activity of 6 was lower or comparable with those presented by AgNO 3[13]. Silver N-heterocyclic carbene complexes are widely described in the literature as effective antibacterial, antifungal, and antiviral agents[1]. Haque et al. synthesized dinuclear silver complexes with N-heterocyclic carbene, which possessed good antibacterial activity. The authors also demonstrated that compounds containing benzimidazole moiety exhibited significantly higher activity than complexes with imidazole[51]. "
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    ABSTRACT: Selected aspects of the biological activity of a series of six nitrate silver(I) complexes with pyridine and (benz)imidazole derivatives were investigated. The present study evaluated the antibacterial activities of the complexes against three Gram-negative strains: Pseudomonas aeruginosa ATCC 15442, Escherichia coli ATCC 25922 and Proteus hauseri ATCC 13315. The results were compared with those of silver nitrate, a silver sulfadiazine drug and appropriate ligands. The most significant antibacterial properties were exerted by silver(I) complexes containing benzimidazole derivatives. The cytotoxic activity of the complexes was examined against B16 (murine melanoma) and 10T1/2 (murine fibroblasts) cells. All of the tested silver(I) compounds were not toxic to fibroblast cells in concentration inhibited cancer cell (B16) viability by 50%, which ranged between 2.44-28.65 µM. The molecular and crystal structure of silver(I) complex of 2,6-di(hydroxymethyl)pyridine was determined by single-crystal X-ray diffraction analysis. The most important features of the crystal packing and intermolecular non-covalent interactions in the Ag(I) complex were quantified via Hirshfeld surface analysis.
    Preview · Article · Jan 2016 · Molecules
    • "For the last 40 years, serious efforts have been made to design and synthesize potential chemotherapeutic agents for anticancer therapy[2,3]. Benzimidazole derivatives have been reported to exhibit antibacterial, antiviral, antiparasitic, anthelmintic , antitumor, anti-inflammatory, antioxidant, antiulcer, antihypertensive, anticoagulant, antidepressant, anticonvulsant , antihistaminic, antiasthmatic, and antidiabetic activities4567. Recently, some benzimidazoles have also been found to have remarkable antileukemic activities8910111213. It is known that Hoechst 33342 and 33258 (Figure 1) are adenine-thymine-specific dyes that stain DNA by binding to its minor groove. "
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    No preview · Article · May 2015 · Zeitschrift fur Naturforschung C
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    • "Several benzophenones are under study; combretastatin A-4 is known to exhibit antiangiogenic effects and is being studied in clinical trials (Tozer et al., 2008). The presence of a benzimidazole nucleus in numerous categories of therapeutic agents has made it an indispensable anchor for the development of new antiangiogenic therapeutics (Yogita and Silakari, 2012). Previously, we reported the synthesis and antitumor and antiangiogenic properties of (2- aroyl-4-methylphenoxy)acetamides 4a–e, which are benzophenone analogs (Prabhakar et al., 2006a, 2006b). "
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