2. Academic Validation
  3. Synthesis and cytotoxicity of novel (thiazol-2-yl)hydrazine derivatives as promising anti-Candida agents

Synthesis and cytotoxicity of novel (thiazol-2-yl)hydrazine derivatives as promising anti-Candida agents

  • Eur J Med Chem. 2013 Jul:65:102-11. doi: 10.1016/j.ejmech.2013.04.042.
Simone Carradori 1,  Daniela Secci,  Adriana Bolasco,  Daniela Rivanera,  Emanuela Mari,  Alessandra Zicari,  Lavinia Vittoria Lotti,  Bruna Bizzarri
Affiliations

Affiliation

  • 1 Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy. simone.carradori@uniroma1.it
PMID: 23702472 DOI: 10.1016/j.ejmech.2013.04.042
Abstract

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.

Keywords

Antifungal drugs; Candida spp.; Cytotoxicity; FIC index; Hantzsch reaction; Thiazole.

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