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The Importance of Rhodanine Scaffold in Medicinal Chemistry: A Comprehensive Overview

Journal

MINI-REVIEWS IN MEDICINAL CHEMISTRY
Volume 21, Issue 6, Pages 738-789

Publisher

BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1389557521666201217144954

Keywords

Rhodanine; biological activity; structure-activity relationship; staffold; medicinal chemistry

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Rhodanine-based compounds have shown broad biological activities through various modifications to the rhodanine ring, making them important in drug discovery.
After the clinical use of epalrestat that contains a rhodanine ring, in type II diabetes mellitus and diabetic complications, rhodanin-based compounds have become an important class of heterocyclic in the field of medicinal chemistry. Various modifications to the rhodanine ring have led to a broad spectrum of biological activity of these compounds. Synthesis of rhodanine derivatives, depended on advenced throughput scanning hits, frequently causes potent and selective modulators of targeted enzymes or receptors, which apply their pharmacological activities through different mechanisms of action. Rhodanine-based compounds will likely stay a privileged scaffold in drug discovery because of different probability of chemical modifications of the rhodanine ring. We have, therefore reviewed their biological activities and structure activity relationship.

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