An overview of benzo [b] thiophene-based medicinal chemistry

Aug 1, 2017European journal of medicinal chemistry

Summary of drug research based on benzo[b]thiophene compounds

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Abstract

Benzothiophene derivatives exhibit a wide range of biological activities, including anti-cancer and anti-inflammatory effects.

Benzothiophene is recognized for its structural similarities to active compounds used in drug development.
Compounds based on the benzo[b]thiophene scaffold have shown potential as anti-microbial, anti-cancer, and anti-diabetic agents.
Numerous benzothiophene derivatives are currently utilized as clinical drugs due to their high therapeutic potency.
Structure activity relationship (SAR) studies have identified specific chemical groups linked to the biological activities of benzothiophene derivatives.
The review aims to summarize pharmacological advancements in benzothiophene derivatives and promote rational drug design.

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Among sulfur containing heterocycles, benzothiophene and its derivatives are at the focus as these candidates have structural similarities with active compounds to develop new potent lead molecules in drug design. Benzo[b]thiophene scaffold is one of the privileged structures in drug discovery as this core exhibits various biological activities allowing them to act as anti-microbial, anti-cancer, anti-inflammatory, anti-oxidant, anti-tubercular, anti-diabetic, anti-convulsant agents and many more. Further, numerous benzothiophene-based compounds as clinical drugs have been extensively used to treat various types of diseases with high therapeutic potency, which has led to their extensive developments. Due to the wide range of biological activities of benzothiophene, their structure activity relationships (SAR) have generated interest among medicinal chemists, and this has culminated in the discovery of several lead molecules against numerous diseases. The present review is endeavoring to highlight the progress in the various pharmacological activities of benzo[b]thiophene derivatives. It is hoped that this review will be helpful for new thoughts in the quest for rational designs of more active and less toxic benzothiophene-based medicinal drugs, as well as more effective diagnostic agents and pathologic probes. Also, SAR studies that highlight the chemical groups responsible for evoking the potential activities of benzothiophene derivatives are studied and compared.

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An overview of benzo [b] thiophene-based medicinal chemistry

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