Thiophenyl-substituted triazolyl-thione L-alanine: asymmetric synthesis, aggregation and biological properties

Amino Acids. 2014 Oct;46(10):2325-32. doi: 10.1007/s00726-014-1782-3. Epub 2014 Jun 22.

Abstract

In this work, we report the asymmetric synthesis and characterization of an artificial amino acid based on triazolyl-thione L-alanine, which was modified with a thiophenyl-substituted moiety, as well as in vitro studies of its nucleic acid-binding ability. We found, by dynamic light scattering studies, that the synthetic amino acid was able to form supramolecular aggregates having a hydrodynamic diameter higher than 200 nm. Furthermore, we demonstrated, by UV and CD experiments, that the heteroaromatic amino acid, whose enzymatic stability was demonstrated by HPLC analysis also after 24 h of incubation in human serum, was able to bind a RNA complex, which is a feature of biomedical interest in view of innovative antiviral strategies based on modulation of RNA-RNA molecular recognition.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alanine / analogs & derivatives*
  • Alanine / chemical synthesis
  • Alanine / chemistry
  • Alanine / metabolism
  • Amino Acids, Aromatic / chemical synthesis*
  • Amino Acids, Aromatic / chemistry
  • Amino Acids, Aromatic / metabolism
  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / chemistry
  • Antiviral Agents / metabolism
  • Circular Dichroism
  • Drug Design*
  • Magnetic Resonance Spectroscopy
  • Molecular Conformation
  • Molecular Structure
  • Nephelometry and Turbidimetry
  • RNA / chemistry
  • RNA / metabolism
  • Spectrometry, Mass, Electrospray Ionization
  • Spectrophotometry, Ultraviolet
  • Thiophenes / chemical synthesis
  • Thiophenes / chemistry*
  • Thiophenes / metabolism
  • Triazoles / chemical synthesis
  • Triazoles / chemistry*
  • Triazoles / metabolism

Substances

  • Amino Acids, Aromatic
  • Antiviral Agents
  • Thiophenes
  • Triazoles
  • RNA
  • Alanine