Design, Synthesis and Antimalarial Activity of Some New Aminoalcoholpyrrolo[1,2-a]quinoxaline Derivatives

Author(s): Jean Guillon, Stéphane Moreau, Luisa Ronga, Louise Basmacyian, Anita Cohen, Sandra Rubio, Guillaume Bentzinger, Solène Savrimoutou, Nadine Azas, Catherine Mullié, Pascal Sonnet.

Journal Name: Letters in Drug Design & Discovery

Volume 13 , Issue 9 , 2016

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Abstract:

Following our search for antimalarial compounds, novel series of piperazinylalcohol pyrrolo[ 1,2-a]quinoxaline derivatives 1-2 were synthesized from 2-nitroaniline or 2-amino-3- nitrophenol and tested for in vitro activity upon the intraerythrocytic stage of W2 and 3D7 Plasmodium falciparum strains. Biological results showed good antimalarial activity with IC50 ranging from 0.3 to 21.1 µM. In attempting to investigate the large broad-spectrum antiprotozoal activities of these pyrrolo[1,2-a]quinoxaline derivatives, their properties toward the promastigote form of Leishmania donovani were also investigated and revealed their selective antiplasmodial profile. In parallel, the in vitro cytotoxicity of these molecules was assessed on the human HepG2 cell line. Structure-activity relationships of these new synthetic compounds are here discussed.

Keywords: Antimalarial activity, pyrrolo[1, 2-a]quinoxaline, synthesis, antileishmanial activity.

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Article Details

VOLUME: 13
ISSUE: 9
Year: 2016
Page: [932 - 942]
Pages: 11
DOI: 10.2174/1570180813666160517164758
Price: $58

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