Synthesis and Antimicrobial Activity of Some New Spiropyrazoline Derivatives of 9α-and 9β-Hydroxyparthenolide

摘要

In the present study,we efficiently synthesized two new series of spiropyrazoline derivatives from 9α-and 9β-hydroxyparthenolide(isolated from the aerial parts of Anvillea radiata).The compounds were obtained by modifications at the C-13 and C-9 positions via 1,3-dipolar cycloaddition followed by O-H acylation at the C1-C10 using epoxidation with metachloroperoxybenzoic acid(m-CPBA)followed by 1,3-dipolar cycloaddition on the double bond α-methylene-γ-lactones.The structures and stereochemistry of the cycloadducts were established by spectroscopic methods,including X-ray diffraction data.Some compounds were tested for antibacterial activity.Several spiropyrazoline derivatives showed good to moderate activity against bacteria.