N -Cinnamoylated Aminoquinolines as Promising Antileishmanial Agents | Zendy

Sílvia Vale-Costa | Zendy; Joana Costa-Gouveia | Zendy; Bianca Pérez | Zendy; Tânia Silva | Zendy; Cátia Teixeira | Zendy; Paula Gomes | Zendy; Maria Salomé Gomes | Zendy

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N -Cinnamoylated Aminoquinolines as Promising Antileishmanial Agents

Author(s) -

Sílvia Vale-Costa,

Joana Costa-Gouveia,

Bianca Pérez,

Tânia Silva,

Cátia Teixeira,

Paula Gomes,

Maria Salomé Gomes

Publication year - 2013

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.00557-13

Subject(s) - primaquine , chloroquine , pharmacology , in vitro , aminoquinolines , chemistry , amastigote , toxicity , leishmania , biology , malaria , biochemistry , combinatorial chemistry , immunology , parasite hosting , organic chemistry , world wide web , computer science

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.

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