Synthesis and Biological Evaluation of Taurine-Derived Diarylmethane and Dibenzoxanthene Derivatives as Possible Cytotoxic and Antimicrobial Agents

Chem Biodivers. 2022 Apr;19(4):e202100970. doi: 10.1002/cbdv.202100970. Epub 2022 Mar 24.

Abstract

The series of novel taurine-derived diarylmethanes and dibenzoxanthenes was synthesized starting from simple commercially available precursors via modular three-stage approach. All the newly synthesized compounds were screened for in vitro antibacterial and antifungal activity, as well as cytotoxicity towards normal and cancer cell lines. Some of the synthesized compounds exhibited 2-4-fold higher activity against S. aureus, E. faecalis and B. cereus compared with Chloramphenicol. In contrast to Chloramphenicol, the tested compounds also showed bactericidal, rather than bacteriostatic effect, which makes them promising candidates for further studies.

Keywords: antimicrobial agents; cytotoxic agents; diarylmethane; dibenzoxanthene; taurine.

MeSH terms

  • Anti-Bacterial Agents / pharmacology
  • Anti-Infective Agents* / pharmacology
  • Antifungal Agents / pharmacology
  • Antineoplastic Agents* / pharmacology
  • Chloramphenicol
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Staphylococcus aureus
  • Structure-Activity Relationship
  • Taurine
  • Xanthenes

Substances

  • Anti-Bacterial Agents
  • Anti-Infective Agents
  • Antifungal Agents
  • Antineoplastic Agents
  • Xanthenes
  • dibenzoxanthenes
  • Taurine
  • Chloramphenicol