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Syntheses of new isodethiaazacephems as potent antibacterial agents
J R Hwu1, S C Tsay, S Hakimelahi
1Organosilicon and Synthesis Laboratory, Institute of Chemistry, Academia Sinica, Nankang, Taipei, Taiwan 11529, Republic of China.
Journal of Medicinal Chemistry
|November 21, 1998
Abstract:
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.