Synthesis and antimalarial activity of 7- benzylamino- 1- isoquinolinamines

Gutteridge, Clare E.; Hoffman, Marshall M.; Bhattacharjee, Apurba K.; Gerena, Lucia

Previous computer modeling has suggested that 7- benzylamino- 1- isoquinolinamines should mediate antimalarial effects by a mechanism distinct from that employed by existing antimalarial drugs.  These compds. were prepd. (e.g. 7- benzylamino- 1- isoquinolinamine dihydrochloride) in seven synthetic steps, via reductive amination of 1, 7- isoquinolinediamine.  In vitro efficacy testing of the novel compds. against Plasmodium falciparum revealed them to be potent antimalarial agents.