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Synthesis and anti-Candida activity of novel 2-hydrazino-1,3-thiazole derivatives
Authors:Ludovic T. Maillard  Sébastien Bertout  Ophélie Quinonéro  Gülşen Akalin  Gülhan Turan-Zitouni  Pierre Fulcrand  Fatih Demirci  Jean Martinez  Nicolas Masurier
Affiliation:1. Institut des Biomole´cules Max Mousseron, UMR 5247, CNRS, Universite´s Montpellier I et II, UFR des Sciences Pharmaceutiques et Biologiques, 15 Avenue Charles Flahault, 34093 Montpellier Cedex 5, France;2. UMI 233 IRD-UM1-UY1-UCAD ‘TransVIHMI’ Equipe Infections parasitaires et fongiques liées au VIH UFR Sciences Pharmaceutiques et Biologiques, 15 Avenue Charles Flahault, BP 14491, 34093 Montpellier Cedex 5, France;3. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eski?ehir, Turkey;4. Department of Biochemistry, Faculty of Pharmacy, Anadolu University, 26470 Eski?ehir, Turkey;5. Department of Pharmacognosy, Faculty of Pharmacy, Anadolu University, 26470 Eski?ehir, Turkey
Abstract:Eighteen new hydrazino-1,3-thiazole derivatives were evaluated against 8 strains of multi-resistant Candida spp. Introduction of an indolyl moiety linked to the hydrazone function enhanced the in vitro anti-Candida activity, with an activity spectrum towards Candida albicans strains. Introduction of a (S)-2-aminoethyl chain on the thiazole nucleus largely enhanced the in vitro antifungal activity, with a selectivity oriented towards non-C. albicans species.
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