Antimicrobial Activity of 3-Substituted Thioxopyrrolidines

抄録

Fifteen 3-substituted thioxopyrrolidines were synthesized and assayed for their antimicrobial activities against Eurotium chevalieri, Schizosaccharomyces pombeand Staphylococcus epidermidis.3- [(α-Alkoxy)-α-methoxy] methyl-(1-7) and 3- [(α-alkoxy)-α-methylthio] met hyl-2-thioxopyrrolidines (8-11) showed antimicrobial activity againstE. chevalieriandS. epidermidis, and their activity increased by lengthening the alkoxyl chain. 3-Alkoxymethylene- 2-thioxopyrrolidines (12-15) were less active against the fungi and the bacteria. For the thioxopyrrolidines, a positive correlation was observed between the hydrophobicity of the compounds and their activities against E. chevalieri. On the other hand, against the yeast, compounds 8-15 behaved differently from 1-7, and the highest activity was associated with the ethoxy (9) and the propoxy (14) derivatives of compounds 8-11 and 12-15, respectively.