Abstract
Benzimidazole is a bicyclic heterocyclic aromatic compound in which benzene fused to imidazole moiety. Benzimidazole holds a vital role in the field of medicinal chemistry which possesses wide variety of pharmacological activities like antibacterial, anti cancer, antifungal, antileishmanial, anti tubercular, anti viral and anti malarial respectively, hence the benzimidazole moiety attracting the medicinal chemist to synthesize the different benzimidazole derivatives with wide variety of pharmacological activities. The book chapter mainly discussed the anti cancer, anti HIV, antileishmanial and anti tubercular activites of recently synthesized benzimidazole derivatives.
Keywords
- benzimidazole
- anti cancer
- anti HIV
- antileishmanial
- anti tubercular
1. Introduction
Benzimidazole is bicyclic heterocyclic aromatic compound in which benzene ring fused to 4 and 5 position of imidazole ring, it contain two nitrogen atoms at 1 and 3 position exhibit both acidic and basic nature called amphotericin nature and exists in two equivalent tautomeric forms, when the hydrogen present at first position nitrogen atom possess acidic nature, when the hydrogen present at third position nitrogen atom possess basic nature (Figures 1) [1]. Benzimidazole is a very important important pharmacophore among all the heterocyclic compounds due to its important pharmacological activities like anti-Alzheimer [2], antibacterial [3], anti cancer [4], anti-diabetic [5], antifungal [6], anti HIV [7], anti leishmanial [8], anti inflammatory [9], analgesic [9], anti malarial [10], anti microbial [11] and anti tubercular [12] activity, there are many benzimidazole derivatives are using to treat many diseases, few presently marketing drugs contain benzimidazole moiety are the bezitramide using as an analgesic, ridinilazole sing as antibacterial, the candesartan, mibefradil using as antihypertensive drugs, mebendazole, albendazole, thiabendazole, and flubendazole usng as antihelminthics, astemizole, bilastine using as antihistamines, pantoprazole, lansoprazole, esomeprazole, ilaprazole using as proton pump inhibitors, bendamustine, selumetinib, galeterone, pracinostat using as antitumor agents and enviradine, samatasvir, and maribavir using as antiviral agents (Figures 2) [13, 14, 15, 16, 17].
2. Pharmacological profile of benzimidazole derivatives
2.1 Anti cancer activity
In the year of 2019 Tahlan et al., reported the synthesis and anti cancer activity of the new benzimidazole derivatives, among all the derivatives the compound
In 2015 few authors worked on synthesis of benzimidazole and evaluated the nti-cancer activit, the Gao et al., reported the compound
In 2014 Yoon et al., evaluated the anti cancer activity of synthesized novel benzimidazole derivatives, the compounds
In 2013 Sharma et al., reported the anti cancer activity of synthesized the benzimidazole quinazoline hybrids, the compound
2.2 Anti HIV activity
In the year of 2020 Srivastava et al., reported the synthesis and anti HIV activity of the new benzimidazole derivatives, among all the derivatives the compound
2.3 Anti leishmanial activity
M. Tonelli et al., reported the antileishmanial activity of newly synthesized benzimidazole derivatives, among all the derivatives compound
2.4 Anti tubercular activity
In the year of 2019 S. Manivannan et al., reported the synthesis anti tubercular activity of benzimidazole derivatives, among all the derivatives compound
In the year of 2014 many authors reported the anti tubercular activity of synthesized the new benzimidazole derivatives, Gong et al., reported the compound
In the year of 2013 also many authors evaluated the anti tubercular activity of newly synthesized benzimidazole derivatives, Nandha et al., reported the compound
In 2012 Patel et al., reported the anti tubercular activity of synthesized the benzimidazolyl-1,3,4-oxadiazol-2ylthio-
In 2011 few authors reported the anti tubercular activity of synthesized benzimidaoles, Saleshier et al., reported the compounds
3. Conclusions
The benimidazole plays in important role in the field of medicinal chemistry, many of the marketing drugs contain benzimidazole moiety are using to illness. In recent medicinal chemistry research the benzimidazole derivatives are in continuous development with many pharmacological activities such as anti-cancer, anti-HIV, anti-leishmanial, anti-tubercular, anti-malarial, anti-inflammatory, anti-diabetic, and so on, to meet pharmacological requirement. The present literature may helpful to researcher, medicinal chemist, pharmacologist to design, to synthesize, to develop pharmacologically active benzimidazole derivatives with low toxicity in future.
Acknowledgments
All the authors are thankful to managements of respective colleges for providing facilities to carry out the work.
Author contribution
Mahender Thatikayala contributed the chemistry, anti cancer, anti leishmanial and anti tubercular activity of benzimidazoles. Anil Kumar Garige, Hemalatha Gadegoni contributed the chemistry and anti HIV activity of benzimidazoles.
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