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Synthesis and Antimicrobial Activity of Thiosulfinates and Allicin Analogues

  • V. M. Puchkov,
  • A. D. Lyfenko,
  • V. S. Koval,
  • S. V. Revtovich,
  • V. V. Kulikova,
  • N. V. Anufrieva,
  • A. S. Zemskaya,
  • E. A. Morozova,
  • P. N. Solyev

摘要

Abstract

Diallyl thiosulfinate (allicin) effectively inhibits the growth of various microorganisms, including antibiotic-resistant strains, so it can be considered to be a broad-spectrum antimicrobial compound. However, its instability in the bloodstream hinders its use as a therapeutic agent. We have synthesized a number of allicin analogues, both natural and synthetic, and evaluated in vitro their antimicrobial properties against Staphylococcus aureus and Candida albicans. The synthesized compounds were shown to exhibited more pronounced antifungal activity than antibacterial. Among the compounds obtained, synthetic di-(2,2,2-trichloroethyl) ester of 3,3'-[(thio)sulfinyl]dipropionic acid effectively inhibited the growth of both fungi and bacteria at concentrations comparable to those of known antimicrobial agents used in medical practice.