Synthesis and Antifungal Potential of Some Novel Benzimidazole-1,3,4-Oxadiazole Compounds

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KARABURUN A. Ç., Cavusoglu B. K., ACAR ÇEVİK U., OSMANİYE D., SAĞLIK B. N., LEVENT S., ...More

MOLECULES, vol.24, no.1, 2019 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 24 Issue: 1
  • Publication Date: 2019
  • Doi Number: 10.3390/molecules24010191
  • Journal Name: MOLECULES
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Keywords: benzimidazole, 1, 3, 4-oxadiazole, antifungal activity, ergosterol biosynthesis, cytotoxicity, molecular docking, BENZIMIDAZOLE DERIVATIVES, ANTIMICROBIAL ACTIVITY, BIOLOGICAL EVALUATION, INHIBITION, ANTICONVULSANT, ANTIBACTERIAL, ANTICANCER, DESIGN, AGENTS
  • Bilecik Şeyh Edebali University Affiliated: No

Abstract

Discovery of novel anticandidal agents with clarified mechanisms of action, could be a rationalist approach against diverse pathogenic fungal strains due to the rise of resistance to existing drugs. In support to this hypothesis, in this paper, a series of benzimidazole-oxadiazole compounds were synthesized and subjected to antifungal activity evaluation. In vitro activity assays indicated that some of the compounds exhibited moderate to potent antifungal activities against tested Candida species when compared positive control amphotericin B and ketoconazole. The most active compounds 4h and 4p were evaluated in terms of inhibitory activity upon ergosterol biosynthesis by an LC-MS-MS method and it was determined that they inhibited ergosterol synthesis concentration dependently. Docking studies examining interactions between most active compounds and lanosterol 14--demethylase also supported the in vitro results.