A review on the synthesis and biological relevance of benzo[b]thiophene derivatives

Heterocyclic compounds occupy a central position in synthetic organic chemistry due to their broad range of applications. The electron-rich sulfur atom of benzo[b]thiophenes with its planar structure enhances the binding affinity with various enzymes and receptors. Since it is a polar compound, it i...

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Bibliographic Details
Published in:Phosphorus, sulfur, and silicon and the related elements sulfur, and silicon and the related elements, 2023-04, Vol.198 (4), p.283-299
Main Authors: Dhanya, T. M., Anjali Krishna, G., Savitha, D. P., Shanty, A. A., Divya, K. M., Priya, Shenoi K., Mohanan, P. V.
Format: Article
Language:English
Subjects:
anti-cancer
anti-leishmanial
anti-microbial
Anticancer properties
Benzothiophene
Bioavailability
Chemical reactions
Chemical synthesis
Heterocyclic compounds
Lewis acid
Microorganisms
Organic chemistry
Oxidizing agents
Planar structures
synthesis
Thiophenes
Toxicity
Transition metals
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Summary:Heterocyclic compounds occupy a central position in synthetic organic chemistry due to their broad range of applications. The electron-rich sulfur atom of benzo[b]thiophenes with its planar structure enhances the binding affinity with various enzymes and receptors. Since it is a polar compound, it improves the pharmacokinetic features of the pilot molecules and it can thus be consequently used as an attractive probe due to low toxicity, high solubility, and bioavailability. This scaffold exhibits numerous biological activities such as anti-microbial, anti-cancer, anti-leishmanial, anti-oxidant, anti-malarial, anti-diabetic, anthelmintic, etc. The common methods used for their synthesis mainly include Lewis acid-catalyzed, halogen-catalyzed, transition metal-catalyzed, base-catalyzed, electrophilic, and acid-catalyzed cyclization reactions. This review examines diverse synthetic methods and biological applications of the reported benzo[b]thiophene derivatives.
ISSN:1042-6507
1563-5325
DOI:10.1080/10426507.2022.2145476