A DIC mediated expeditious small library synthesis and biological activity of thiazolidin-4-one and 1,3-thiazinan-4-one derivatives

✍ Scribed by Amit Verma; Shweta S Verma; Shailendra K Saraf

• Publisher: Journal of Heterocyclic Chemistry
• Year: 2010
• Tongue: English
• Weight: 183 KB
• Volume: 47
• Category: Article
• ISSN: 0022-152X
• DOI: 10.1002/jhet.429

✦ Synopsis

Abstract

magnified image A diisopropylcarbodiimide (DIC) mediated small library of thiazolidin‐4‐one and 1,3‐Thiazinan‐4‐one derivatives were efficiently synthesized using one pot three component condensation of amino acid, aldehyde, and mercapto carboxylic acid on a polymer support. The study shows significantly higher yields of the thiazolidin‐4‐one derivatives thereby indicating a lower dependence on the nature of the amino acid and aldehyde components. As an obvious extension of this protocol, the reactions were performed using heterocyclic aldehydes and substituted hindered aromatic aldehydes instead of simple aromatic aldehydes. The synthesized library compounds were also screened for their antifungal acitivity against these three pathogenic fungi: Candida albicans (Ca), Candida parapsilosis (Cp), and Cryptococcus neoformans (Cn). J. Heterocyclic Chem., (2010).