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

Abstract

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).

Keywords: shikimic acid, epoxide ring opening, influenza, oseltamivir, oseltamivir phosphate, Tamiflu, anti-Herpes simplex virus type-1, anti-alzheimer, anti-tyrosinase activity and cytotoxicity.