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Benzimidazole: a medicinally important heterocyclic moiety

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TLDR
Researchers have synthesized variety of benzimidazole derivatives and screened them for their various biological activities, viz., anticancer, hormone antagonist, antiviral, anti-HIV, anthelmintic, antiprotozoal, antimycobacterial, antihypertensive, pro-inflammatory, analgesic, anxiolytic, antiallergic, coagulant, anticoagULant, antioxidant as well antidiabetic activities.
Abstract
Benzimidazole nucleus is a constituent of many bioactive heterocyclic compounds that are of wide interest because of their diverse biological and clinical applications. Moreover, benzimidazole derivatives are structural isosters of naturally occurring nucleotides, which allows them to interact easily with the biopolymers of the living system. This created interest in researchers who have synthesized variety of benzimidazole derivatives and screened them for their various biological activities, viz., anticancer, hormone antagonist, antiviral, anti-HIV, anthelmintic, antiprotozoal, antimycobacterial, antihypertensive, anti-inflammatory, analgesic, anxiolytic, antiallergic, coagulant, anticoagulant, antioxidant as well antidiabetic activities.

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Citations
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Journal ArticleDOI

The therapeutic journey of benzimidazoles: a review.

TL;DR: 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 benzimdazole derived compounds for each activity.
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A versatile approach to Ullmann C-N couplings at room temperature: new families of nucleophiles and electrophiles for photoinduced, copper-catalyzed processes.

TL;DR: The use of light to facilitate copper-catalyzed cross-couplings of nitrogen nucleophiles can enable C-N bond formation to occur under unusually mild conditions.
Journal ArticleDOI

Design, synthesis and biological evaluation of 1,3-diphenyl-1H-pyrazole derivatives containing benzimidazole skeleton as potential anticancer and apoptosis inducing agents.

TL;DR: A series of forty different pyrazole containing benzimidazole hybrids have been designed, synthesized and evaluated for their potential anti-proliferative activity against three human tumor cell lines - lung, breast, and cervical.
Journal ArticleDOI

Design, synthesis and antimicrobial evaluation of novel benzimidazole type of Fluconazole analogues and their synergistic effects with Chloromycin, Norfloxacin and Fluconazole

TL;DR: The bioactive evaluation showed that 3,5-bis(trifluoromethyl)phenyl benzimidazoles gave comparable or even stronger antibacterial and antifungal efficiency in comparison with reference drugs Chloromycin, Norfloxacin and Fluconazole.
References
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Journal ArticleDOI

Synthesis and anticancer evaluation of bis(benzimidazoles), bis(benzoxazoles), and benzothiazoles.

TL;DR: Four classes of UK-1 analogues were synthesized and their cytotoxicity testing against human A-549, BFTC-905, RD, MES-SA, and HeLa carcinoma cell lines was determined, revealing that these analogues are potent against the cancer cell lines.
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Synthesis and Evaluation of Anticancer Benzoxazoles and Benzimidazoles Related to UK-1

TL;DR: Results support a role of Mg(2+) ion binding in the selective cytotoxicity of UK-1 and provide a minimal pharmacophore for the select cytotoxic activity of the natural product.
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Synthesis of some new 2-substituted-phenyl-1H-benzimidazole-5-carbonitriles and their potent activity against Candida species.

TL;DR: New 2-substituted-phenyl-1H-benzimidazole-5-carboxylic acids, and cyano substituted compounds 53, 57, 58 and 61 exhibited the greatest activity with MIC values similar to that of fluconazole.
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2-dimethylamino-4,5,6,7-tetrabromo-1H-benzimidazole: a novel powerful and selective inhibitor of protein kinase CK2

TL;DR: A novel compound, 2-dimethylamino-4,5,6,7-tetrabromo-1H-benzimidazole (DMAT), is described, which is superior to the commonly used specific CK2 inhibitor 4, 5, 6, 7-t Petrabromobenzotriazoles (TBB) in several respects and is the first choice CK2 inhibitors for in vivo studies available to date.
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Synthesis, antiviral and antitumor activity of 2-substituted-5-amidino-benzimidazoles

TL;DR: Interestingly, all compounds show noticeable selectivity toward breast cancer cell line MCF-7, and the most distinct and selective antiviral activity toward coxsackieviruses and echoviruses was observed with compounds having pyridine ring at C-2.
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