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[摘要]: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). |
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