First synthesis and antimicrobial activity Of N- and S-alpha-L-arabinopyranosyl-1,2,4-triazoles

Nucleosides Nucleotides Nucleic Acids. 2007;26(4):361-77. doi: 10.1080/15257770701296986.

Abstract

Arabinosylation of some 4-amino- and 4-arylideneamino-5-(pyridin-3-yl)-2,4-dihydro-[1,2,4]-triazole-3-thiones with 2,3,4-tri-O-acetyl-beta-L-arabinopyranosyl bromide led to an efficient synthetic approach to the corresponding N-and S-alpha-L-arabinopyranosides. Structure assignment of these two regiosiomers was based on chemical and spectroscopic evidences. Antimicrobial activities of two selected regioisomeric N-and S-alpha-L-arabinopyranosides were compared. The N-alpha-L-arabinopyranoside showed higher inhibitory effect than its regioisomeric S-alpha-L-arabinopyranoside against Aspergillus fumigatus, Penicillium italicum, Staphylococcus aureus, and Pseudomonas aeruginosa.

MeSH terms

  • Anti-Infective Agents / chemical synthesis*
  • Anti-Infective Agents / pharmacology
  • Aspergillus fumigatus / growth & development
  • Microbial Sensitivity Tests
  • Penicillium / growth & development
  • Pseudomonas aeruginosa / growth & development
  • Staphylococcus aureus / growth & development
  • Triazoles / chemical synthesis*
  • Triazoles / pharmacology

Substances

  • Anti-Infective Agents
  • Triazoles