Synthesis and Biological activities of Oseltamivir phosphate (Tamiflu), Oseltamivir and Its Derivatives

摘要

Oseltamivir phosphate or Tamiflu TM 1 , oseltamivir 2 and three new oseltamivir derivatives 11-13 were synthesized starting from (-)-shikimic acid 3 . The title compounds were evaluated for their anti-Herpes simplex virus type-1, anti-alzheimer , anti-tyrosinase activity and cytotoxicity. Compound 12 exhibited inhibitory acitivity of HSV-1, AChE, tyrosinase and revealed cytotoxicity against small-cell lung cancer (NCI-H187) cells and Vero cells (African green monkey kidney).