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.