Synthesis and antiviral activity of metabolites of rimantadine

…, E Keech, RB Belshe, EV Connell, IS Sim

Index: Manchand; Cerruti; Martin; Hill; Merrett; Keech; Belshe; Connell; Sim Journal of Medicinal Chemistry, 1990 , vol. 33, # 7 p. 1992 - 1995

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Citation Number: 29

Abstract

The hydroxy metabolites of rimantadine (3-5) were synthesized and compared to amantadine (1) and rimantadine (2) for their ability to inhibit the replication of influenza viruses in vitro. All three metabolites were inhibitory to wild-type influenza A viruses (H3N2 and H1N1). In particular, 2-hydroxyrimantadine (3) showed similar activity to amantadine, but the 3-and 4-hydroxy metabolites (4 and 5, respectively), both of which are found in ...