Benzimidazole-core as an antimycobacterial agent

Within the vast range of heterocycles, benzimidazole and its derivatives are found to be trendy structures employed for discovery of drugs in the field of pharmaceutical and medicinal chemistry. The unique structural features of benzimidazole and a wide range of biological activities of its derivati...

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Veröffentlicht in:Pharmacological reports 2016-12, Vol.68 (6), p.1254-1265
Hauptverfasser: Keri, Rangappa S., Rajappa, Chethana Kolambae, Patil, Siddappa A., Nagaraja, Bhari Mallanna
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container_end_page 1265
container_issue 6
container_start_page 1254
container_title Pharmacological reports
container_volume 68
creator Keri, Rangappa S.
Rajappa, Chethana Kolambae
Patil, Siddappa A.
Nagaraja, Bhari Mallanna
description Within the vast range of heterocycles, benzimidazole and its derivatives are found to be trendy structures employed for discovery of drugs in the field of pharmaceutical and medicinal chemistry. The unique structural features of benzimidazole and a wide range of biological activities of its derivatives made it privileged structure in drug discovery. The related research and developments of benzimidazole based medicinal chemistry has become a rapidly developing and increasingly active topic. Subsequently, for TB there is an urgent need for the development of new drug molecules with newer targets and with an alternative mechanism of action. To pave the way for future research, there is a need to collect the latest information in this promising area. In the present review we have collected published reports on this versatile core to provide an insight so that its full therapeutic potential can be utilized for the treatment of tuberculosis. It is hoped that this review will be helpful for new thoughts in the quest for rational designs of more active and less toxic benzimidazole-based anti-TB drugs. [Display omitted] •Benzimidazole core is an attractive target for drug development.•In this review we discussed benzimidazole as antitubercular agent.•Review analyzes structural requirements of benzimidazole as anti-TB agents, with SAR study.•Review will be helpful for new thoughts in the quest for rational designs anti-TB drugs. Mycobacterium tuberculosis (Mtb) is considered as one of the precarious bacterial infections around the world. Through a projected 8.7 million new tuberculosis (TB) cases and 1.4 million mortalities per annum, this deadly infection resulted insubstantial amount of human deaths than any other single organism bacterial infections. TB is one of India’s most threatening human health problems and it accounts for approximately 33% of the global health issues. Subsequently, for TB there is an imperative need for the improvement of existing drug candidates with newer targets and specified mechanism of action. Within the wide spectra of heterocycles, benzimidazole and its substituted analogues were evidenced promising biological efficacies enabling them to perform as new drug or prodrug candidates. Exceptional structural features of this class of heterocycle and versatile biological applications made it a privileged structural backbone in new drug design and discovery. Majorly, 2,5- and 2,6-disubstituted benzimidazole derivatives shown to induce sig
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Through a projected 8.7 million new tuberculosis (TB) cases and 1.4 million mortalities per annum, this deadly infection resulted insubstantial amount of human deaths than any other single organism bacterial infections. TB is one of India’s most threatening human health problems and it accounts for approximately 33% of the global health issues. Subsequently, for TB there is an imperative need for the improvement of existing drug candidates with newer targets and specified mechanism of action. Within the wide spectra of heterocycles, benzimidazole and its substituted analogues were evidenced promising biological efficacies enabling them to perform as new drug or prodrug candidates. Exceptional structural features of this class of heterocycle and versatile biological applications made it a privileged structural backbone in new drug design and discovery. Majorly, 2,5- and 2,6-disubstituted benzimidazole derivatives shown to induce significant antiTB potential. 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Rep</stitle><addtitle>Pharmacol Rep</addtitle><date>2016-12-01</date><risdate>2016</risdate><volume>68</volume><issue>6</issue><spage>1254</spage><epage>1265</epage><pages>1254-1265</pages><issn>1734-1140</issn><eissn>2299-5684</eissn><abstract>Within the vast range of heterocycles, benzimidazole and its derivatives are found to be trendy structures employed for discovery of drugs in the field of pharmaceutical and medicinal chemistry. The unique structural features of benzimidazole and a wide range of biological activities of its derivatives made it privileged structure in drug discovery. The related research and developments of benzimidazole based medicinal chemistry has become a rapidly developing and increasingly active topic. Subsequently, for TB there is an urgent need for the development of new drug molecules with newer targets and with an alternative mechanism of action. To pave the way for future research, there is a need to collect the latest information in this promising area. In the present review we have collected published reports on this versatile core to provide an insight so that its full therapeutic potential can be utilized for the treatment of tuberculosis. It is hoped that this review will be helpful for new thoughts in the quest for rational designs of more active and less toxic benzimidazole-based anti-TB drugs. [Display omitted] •Benzimidazole core is an attractive target for drug development.•In this review we discussed benzimidazole as antitubercular agent.•Review analyzes structural requirements of benzimidazole as anti-TB agents, with SAR study.•Review will be helpful for new thoughts in the quest for rational designs anti-TB drugs. Mycobacterium tuberculosis (Mtb) is considered as one of the precarious bacterial infections around the world. Through a projected 8.7 million new tuberculosis (TB) cases and 1.4 million mortalities per annum, this deadly infection resulted insubstantial amount of human deaths than any other single organism bacterial infections. TB is one of India’s most threatening human health problems and it accounts for approximately 33% of the global health issues. Subsequently, for TB there is an imperative need for the improvement of existing drug candidates with newer targets and specified mechanism of action. Within the wide spectra of heterocycles, benzimidazole and its substituted analogues were evidenced promising biological efficacies enabling them to perform as new drug or prodrug candidates. Exceptional structural features of this class of heterocycle and versatile biological applications made it a privileged structural backbone in new drug design and discovery. Majorly, 2,5- and 2,6-disubstituted benzimidazole derivatives shown to induce significant antiTB potential. 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subjects 2,5-/2,6-Disubstituted benzimidazole
Animals
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacology
Anti-Bacterial Agents - therapeutic use
AntiTB agents
Antitubercular Agents - chemistry
Antitubercular Agents - pharmacology
Antitubercular Agents - therapeutic use
Benzimidazoles - chemistry
Benzimidazoles - pharmacology
Benzimidazoles - therapeutic use
Drug Design
Drug Safety and Pharmacovigilance
Humans
Medicinal chemistry
Multistep synthesis
Mycobacterium tuberculosis
Mycobacterium tuberculosis - drug effects
Mycobacterium tuberculosis - physiology
Pharmacotherapy
Pharmacy
Review Article
Tubercle bacillus
Tuberculosis - drug therapy
title Benzimidazole-core as an antimycobacterial agent
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