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Review
. 2022 Apr 5:2022:7255299.
doi: 10.1155/2022/7255299. eCollection 2022.

Synthesis of Benzimidazole-Sulfonyl Derivatives and Their Biological Activities

Affiliations
Review

Synthesis of Benzimidazole-Sulfonyl Derivatives and Their Biological Activities

Endale Mulugeta et al. Biochem Res Int. .

Abstract

Currently, the synthesis of new compounds with potential bioactivities has become a central issue in the drug discovery arena. Among these new compounds, benzimidazole-sulfonyl scaffolds have vital applications in the fields of pharmaceuticals industries. Benzimidazole and sulfonyl compounds have remarkable biological activities, such as antibacterial, antifungal, anti-inflammatory, antiproliferative, carbonic anhydrase inhibitory, and α-amylase inhibitory activities. Furthermore, recent literature mentions the synthesis and bioactivities of some benzimidazole-sulfonyl hybrids. In this review, we focus on reviewing the synthesis of these hybrid scaffolds and their various types of biological activities of the compounds.

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Conflict of interest statement

The authors declare that they have no conflicts of interest.

Figures

Figure 1
Figure 1
Chemical structure of benzimidazole-sulfonyl derivatives.
Figure 2
Figure 2
Chemical structures of sulfa drugs derivatives.
Figure 3
Figure 3
Chemical structures of antibacterial active benzimidazole-sulfonyl derivatives.
Scheme 1
Scheme 1
Synthetic scheme towards compound 14.
Scheme 2
Scheme 2
Synthetic routes towards 1, 2, 3-triazole benzimidazole-sulfonyl derivatives.
Scheme 3
Scheme 3
Synthetic routes towards compound 24.
Scheme 4
Scheme 4
Synthetic routes towards compound 27.
Scheme 5
Scheme 5
Synthetic routes towards compound 30.
Scheme 6
Scheme 6
Synthetic routes towards compound 35.
Scheme 7
Scheme 7
Synthetic routes towards compound 45.
Scheme 8
Scheme 8
Synthetic routes towards compound 53 derivatives.
Scheme 9
Scheme 9
Synthetic routes towards compounds 57–59.
Scheme 10
Scheme 10
Synthetic routes towards compound 63 derivatives.
Scheme 11
Scheme 11
Synthetic routes toward compound 69 derivatives.
Scheme 12
Scheme 12
Synthetic routes towards compound 7.
Figure 4
Figure 4
Chemical structures of antifungal active benzimidazole-sulfonyl derivatives.
Figure 5
Figure 5
Chemical structures of antiviral active benzimidazole-sulfonyl derivatives.
Figure 6
Figure 6
Chemical structures of antiproliferative active benzimidazole-sulfonyl derivatives.
Figure 7
Figure 7
Chemical structures of anti-inflammatory active benzimidazole-sulfonyl derivatives.
Figure 8
Figure 8
Chemical structures of anti-inflammatory active benzimidazole-sulfonyl derivatives.
Figure 9
Figure 9
Chemical structures of carbonic anhydrases inhibitors active benzimidazole-sulfonyl derivatives.
Figure 10
Figure 10
Chemical structure of α-amylase inhibitory active benzimidazole-sulfonamide derivative.

References

    1. Breijyeh Z., Jubeh B., Karaman R. Resistance of gram-negative bacteria to current antibacterial agents and approaches to resolve it. Molecules . 2020;25(6) doi: 10.3390/molecules25061340.1340 - DOI - PMC - PubMed
    1. Thakral S., Singh V. Recent development on importance of heterocyclic amides as potential bioactive molecules: a review. Current Bioactive Compounds . 2019;15(3):316–336. doi: 10.2174/1573407214666180614121140. - DOI
    1. Aragón-Muriel A., Liscano Y., Upegui Y., et al. In vitro evaluation of the potential pharmacological activity and molecular targets of new benzimidazole-based Schiff base metal complexes. Antibiotics . 2021;10(6):p. 728. doi: 10.3390/antibiotics10060728. - DOI - PMC - PubMed
    1. Karaburun A. Ç., Kaya Çavuşoğlu B., Acar Çevik U., et al. Synthesis and antifungal potential of some novel benzimidazole-1,3,4-oxadiazole compounds. Molecules . 2019;24(1):p. 191. doi: 10.3390/molecules24010191. - DOI - PMC - PubMed
    1. Zhang H.-Z., He S.-C., Peng Y.-J., et al. Design, synthesis and antimicrobial evaluation of novel benzimidazole-incorporated sulfonamide analogues. European Journal of Medicinal Chemistry . 2017;136:165–183. doi: 10.1016/j.ejmech.2017.04.077. - DOI - PubMed

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