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Synthesis and antimalarial activity of 7‐benzylamino‐1‐isoquinolinamines
Author(s) -
Gutteridge Clare E.,
Hoffman Marshall M.,
Bhattacharjee Apurba K.,
Gerena Lucia
Publication year - 2007
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570440319
Subject(s) - chemistry , plasmodium falciparum , reductive amination , in vitro , antimalarial agent , combinatorial chemistry , stereochemistry , pharmacology , malaria , biochemistry , medicine , immunology , biology , catalysis
Computer modelling suggests that 7‐benzylamino‐1‐isoquinolinamines should mediate antimalarial effects by a mechanism distinct from that employed by existing antimalarial drugs. A series of these compounds was prepared in seven synthetic steps, via reductive amination of 1,7‐isoquinolinediamine. In vitro efficacy testing of the novel compounds against Plasmodium falciparum revealed them to be potent antimalarial agents.