Synthesis and microbial inhibition study of novel 5-imidazolyl substituted isoxazolidines

Cycloaddition of C-imidazolyl-N-phenylnitrotles with monosubstituted alkenes afforded 5-imidazolyl substituted isoxazolidines with high regioselectivity. Novel isoxazolidines were screened for their antibacterial activities against S. aureus, E. coli and B. subtilis by using streptomycin as a positive control. They were also tested for their antifungal activities against E moniliforme, A. niger and C. acremonium by using nystatin as a positive control. Isoxazolidines, 4a and 4f exhibited more potent inhibition towards antifungal activity than the other isoxazolidines prepared. (C) 2004 Elsevier Ltd. All rights reserved.