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2000
Volume 23, Issue 1
  • ISSN: 1570-193X
  • E-ISSN: 1875-6298

Abstract

Thiazolidinones and their 5-ene derivatives have become pivotal in organic and medicinal chemistry due to their diverse pharmacological potential. These compounds have been widely explored for their therapeutic applications, with thiazolidine-based frameworks yielding numerous biologically active molecules. This review consolidates various synthetic approaches to thiazolidinone and 5-ene derivatives, including core modifications, one-pot or multistage syntheses, and transformations of related heterocycles. The manuscript highlights key pharmacological targets of thiazolidinones, ranging from initial hit compounds to fully developed drugs. Specifically, thiazolidinone-rhodanines often appear as frequent hitters or pan-assay interference compounds in high-throughput screens. Studies have shown that modifications at the C5 carbon, particularly through the addition of a 5-ene fraction, enhance the pharmacological profile of these compounds. Additionally, the review addresses substitutions at the C5 and N3 positions, including 5-ene and carboxyl groups, and discusses the biological utility of these modifications. Integrating pharmacologically active groups within a heterocyclic system often results in enhanced bioactivity. The review highlights innovative synthetic strategies for thiazolidinone derivatives, emphasizing the potential of these compounds to explore a broad spectrum of biological activities through structural diversity and targeted modifications.

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/content/journals/mroc/10.2174/0118756298368489250325083742
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A Comprehensive Review on Thiazolidinones and their 5-ene Derivatives: Synthetic Methodologies and Pharmacological Profiles
Mini-Reviews in Organic Chemistry 23, 32 (2026); https://doi.org/10.2174/0118756298368489250325083742
/content/journals/mroc/10.2174/0118756298368489250325083742
/content/journals/mroc/10.2174/0118756298368489250325083742
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  • Article Type:     Review Article
Keyword(s): anti-HIV; anticancer; antifungal; pharmacological; profiles; rhodanines; Thiazolidinones

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