Article

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

ABSTRACT

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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    • "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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