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Tandem synthesis and in vitro antiplasmodial evaluation of new naphtho[2,1-d] thiazole derivatives

Abstract : A series of naphtho[2,1-d]thiazoles was prepared in good yields under microwave irradiation with an original protocol combining tandem direct arylation and intramolecular Knoevenagel reaction on 1,3-thiazole derivatives. Antiplasmodial evaluation of this series highlighted two hit compounds (compounds 11 and 13) displaying promising in vitro activity on the multiresistant K1 Plasmodium falciparum strain. Structure-toxicity and structure activity relationships are also discussed and reveal the importance of the R-1 and R-4 substituents of the naphthyl moiety for the biological profile of the series. (C) 2012 Elsevier Masson SAS. All rights reserved.
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https://hal-amu.archives-ouvertes.fr/hal-01460344
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Submitted on : Tuesday, February 7, 2017 - 4:34:53 PM
Last modification on : Wednesday, August 19, 2020 - 12:08:12 PM

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Anita Cohen, Pierre Verhaeghe, Maxime D. Crozet, Sébastien Hutter, Pascal Rathelot, et al.. Tandem synthesis and in vitro antiplasmodial evaluation of new naphtho[2,1-d] thiazole derivatives. European Journal of Medicinal Chemistry, Elsevier, 2012, 55, pp.315--324. ⟨10.1016/j.ejmech.2012.07.034⟩. ⟨hal-01460344⟩

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