The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species


Çavuşoğlu B., YURTTAŞ L., CANTÜRK Z.

European Journal of Medicinal Chemistry, cilt.144, ss.255-261, 2018 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 144
  • Basım Tarihi: 2018
  • Doi Numarası: 10.1016/j.ejmech.2017.12.020
  • Dergi Adı: European Journal of Medicinal Chemistry
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.255-261
  • Anahtar Kelimeler: Anticandidal, Apoptosis, Cytotoxicity, Oxadiazole, Triazole
  • Bilecik Şeyh Edebali Üniversitesi Adresli: Hayır

Özet

In search of potent and safe antifungal agents, herein, we report the synthesis, characterization and biological activities of triazole-oxadiazole compounds. The structural verification of the molecules was carried out by 1H NMR, 13C NMR and mass spectral data. The in vitro antifungal and apoptotic activity were investigated against C. albicans, C. parapsilosis, C. krusei and C. glabrata. The compounds namely N-(4-nitrophenyl)-2-[(5-(2-((4-methyl-4H-1,2,4-triazol-3-yl)thio)ethyl)-1,3,4-oxadiazol-2-yl)thio]acetamide (4e) and N-(6-fluorobenzothiazol-2-yl)-2-[(5-(2-((4-methyl-4H-1,2,4-triazol-3-yl)thio)ethyl)-1,3,4-oxadiazol-2-yl)thio]acetamide (4i) were detected as the most potent compounds against C. albicans and C. glabrata (MIC90 = 62.5 μg/mL). According to studies on their mechanism of action, it was confirmed that compound 4i has apoptotic effect on four Candida via Annexin V-PI with flow cytometry. The MTT assay revealed that all compounds were determined to be non-toxic against healthy cells in the tested concentrations.