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Synthesis and anti-Candida activity of novel 2-hydrazino-1,3-thiazole derivatives
Journal article   Peer reviewed

Synthesis and anti-Candida activity of novel 2-hydrazino-1,3-thiazole derivatives

Ludovic Maillard, Sébastien Bertout, Ophélie Quinonéro, Gülşen Akalin, Gülhan Turan-Zitouni, Pierre Fulcrand, Fatih Demirci, Jean Martinez and Nicolas Masurier
Bioorganic and Medicinal Chemistry Letters, Vol.23(6), pp.1803-1807
03/2013
PMID: 23403080

Abstract

Animals Antifungal Agents Thiazoles Candida Candida albicans Cell Survival Drug Resistance, Fungal Mice Microbial Sensitivity Tests NIH 3T3 Cells Structure-Activity Relationship
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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