title: N-cinnamoylated aminoquinolines as promising antileishmanial agents.
abstract: A series of cinnamic acid conjugates of primaquine and chloroquine were evaluated for their in vitro antileishmanial activities. Although primaquine derivatives had modest activity, chloroquine conjugates exhibited potent activity against both promastigotes (50% inhibitory concentration [IC50] = 2.6 to 21.8 μM) and intramacrophagic amastigotes (IC50 = 1.2 to 9.3 μM) of Leishmania infantum. Both the high activity of these chloroquine analogues and their mild-to-low toxicity toward host cells make them promising leads for the discovery of new antileishmanial agents.
authors.affiliation: IBMC-Instituto de Biologia Molecular e Celular, Universidade do Porto, Porto, Portugal.
authors.forename: S
authors.initials: S
authors.lastname: Vale-Costa
authors.forename: J
authors.initials: J
authors.lastname: Costa-Gouveia
authors.forename: B
authors.initials: B
authors.lastname: Pérez
authors.forename: T
authors.initials: T
authors.lastname: Silva
authors.forename: C
authors.initials: C
authors.lastname: Teixeira
authors.forename: P
authors.initials: P
authors.lastname: Gomes
authors.forename: M S
authors.initials: MS
authors.lastname: Gomes
mesh_terms: D000634:Aminoquinolines / Q000494:pharmacology; D000981:Antiprotozoal Agents / Q000494:pharmacology*; D002738:Chloroquine / Q000494:pharmacology; D007891:Leishmania / Q000187:drug effects*; D011319:Primaquine / Q000494:pharmacology
chemical_list: D000634:Aminoquinolines; D000981:Antiprotozoal Agents; D002738:Chloroquine; D011319:Primaquine
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