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Review
. 2021 Nov 3:12:762807.
doi: 10.3389/fphar.2021.762807. eCollection 2021.

A Comprehensive Account on Recent Progress in Pharmacological Activities of Benzimidazole Derivatives

Shejuti Rahman Brishty  1 , Md Jamal Hossain  2 , Mayeen Uddin Khandaker  3 , Mohammad Rashed Iqbal Faruque  4 , Hamid Osman  5 , S M Abdur Rahman  1
Affiliations
Review

A Comprehensive Account on Recent Progress in Pharmacological Activities of Benzimidazole Derivatives

Shejuti Rahman Brishty et al. Front Pharmacol. .

Abstract

Nowadays, nitrogenous heterocyclic molecules have attracted a great deal of interest among medicinal chemists. Among these potential heterocyclic drugs, benzimidazole scaffolds are considerably prevalent. Due to their isostructural pharmacophore of naturally occurring active biomolecules, benzimidazole derivatives have significant importance as chemotherapeutic agents in diverse clinical conditions. Researchers have synthesized plenty of benzimidazole derivatives in the last decades, amidst a large share of these compounds exerted excellent bioactivity against many ailments with outstanding bioavailability, safety, and stability profiles. In this comprehensive review, we have summarized the bioactivity of the benzimidazole derivatives reported in recent literature (2012-2021) with their available structure-activity relationship. Compounds bearing benzimidazole nucleus possess broad-spectrum pharmacological properties ranging from common antibacterial effects to the world's most virulent diseases. Several promising therapeutic candidates are undergoing human trials, and some of these are going to be approved for clinical use. However, notable challenges, such as drug resistance, costly and tedious synthetic methods, little structural information of receptors, lack of advanced software, and so on, are still viable to be overcome for further research.

Keywords: anti-infectious; anti-proliferative; cardiovascular agents; diverse pharmacological activities; nitrogenous heterocyclic compounds; structure-activity relationship (SAR).

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Conflict of interest statement

The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest.

Figures

FIGURE 1
FIGURE 1
Diverse biological activities of benzimidazole derivatives.
FIGURE 2
FIGURE 2
1H-benzimidazole and some benzimidazole containing drugs.
FIGURE 3
FIGURE 3
Benzimidazole derivatives with antimicrobial activity.
FIGURE 4
FIGURE 4
Benzimidazole derivatives with antiviral activity.
FIGURE 5
FIGURE 5
Benzimidazole derivatives with anti-inflammatory and analgesic activity.
FIGURE 6
FIGURE 6
Structure activity relationship (SAR) of benzimidazole derivatives having anti-inflammatory activity. The figure represents the SAR studies accomplished by Bukhari et al. (2016).
FIGURE 7
FIGURE 7
Benzimidazole derivatives with antiulcer activity.
FIGURE 8
FIGURE 8
Benzimidazole derivatives with antioxidant activity.
FIGURE 9
FIGURE 9
Structure activity relationship (SAR) of benzimidazole derivatives having antioxidant potentiality. The figure represents the SAR studies accomplished by Baldisserotto et al. (2020).
FIGURE 10
FIGURE 10
Benzimidazole derivatives with anticancer activity.
FIGURE 11
FIGURE 11
Structure activity relationship (SAR) of benzimidazole derivatives having anticancer potentiality. The figure represents the SAR studies accomplished by Song, J. et al. (2019).
FIGURE 12
FIGURE 12
Benzimidazole derivatives with antitubercular activity.
FIGURE 13
FIGURE 13
Structure activity relationship (SAR) of benzimidazole derivatives having anti-tubercular effects. The figure represents the SAR studies accomplished by Gobis et al. (2015).
FIGURE 14
FIGURE 14
Benzimidazole derivatives with antiprotozoal activity.
FIGURE 15
FIGURE 15
Structure activity relationship (SAR) of benzimidazole derivatives effective against Trypanosoma brucei. The figure represents the SAR studies accomplished by Popov et al. (2020).
FIGURE 16
FIGURE 16
Benzimidazole derivatives with antihypertensive activity.
FIGURE 17
FIGURE 17
Benzimidazole derivatives with antidiabetic activity.
FIGURE 18
FIGURE 18
Benzimidazole derivatives with anticoagulant activity.
FIGURE 19
FIGURE 19
Benzimidazole derivatives with anticonvulsant activity.
FIGURE 20
FIGURE 20
Benzimidazole derivatives as neuro-protective agents.
FIGURE 21
FIGURE 21
Benzimidazole derivatives with miscellaneous activities.
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