摘要
New isodethiaazacephems (±)-3, (±)-4, and (±)-10 as well as the 4- sulfonylated isodethiaazacepham (±)-5 were synthesized by chemical methods and found to possess biological activity against five pathogenic microorganisms in vitro. The mesylate and the triflate functionalities in (±)-3 and (±)-4, acting as effective leaving groups, enhanced remarkably the biological activity in comparison with the parent 3- hydroxyisodethiaazacephem (±)-10. The mode of action related to (±)-3 and (±)-4 can be explained by a [1,4]-elimination process.