Synthesis and cytotoxicity of novel (thiazol-2-yl)hydrazine derivatives as promising anti-Candida agents
作者:Simone Carradori、Daniela Secci、Adriana Bolasco、Daniela Rivanera、Emanuela Mari、Alessandra Zicari、Lavinia Vittoria Lotti、Bruna Bizzarri
DOI:10.1016/j.ejmech.2013.04.042
日期:2013.7
Thirty-eight new (4-(4-substituted-phenyl/2,4-disubstituted-phenyl)-thiazol-2-yl)hydrazine derivatives were synthesized in good yield and assayed for their in vitro anti-Candida activity, compared to topical and systemic antifungal drugs, against twenty-two clinical isolates of Candida spp. The concurrent presence of aliphatic chains or cycloaliphatic rings at N1-hydrazine and a 4-methyl/4-methoxyphenyl at C4 position of the thiazole nucleus exhibited an interesting anti-Candida inhibitory activity. Moreover, some of the most active compounds showed synergistic antifungal effects and lower cell toxicity when combined with clotrimazole. (C) 2013 Elsevier Masson SAS. All rights reserved.