Year 2019

• Modyfikacje chemiczne Amfoterycyny B i Nystatyny A1

  Publication

  • K. Skarbek

  - Year 2019

  W ramach badań, opisanych w niniejszej rozprawie doktorskiej, przetestowano możliwości chemicznej modyfikacji części aminocukrowej aglikonu amfoterycyny B i nystatyny A1. Otrzymano chroniony aglikon AmB, posiadający grupę hydroksylową na atomie węgla C19, który posłużył jako substrat w reakcji substytucji nukleofilowej oraz dehydracyjnej glikozylacji. Opracowano i zoptymalizowano warunki syntezy chronionych pochodnych cukrowych,...

  Full text available to download

Year 2018

• Molecular Umbrellas Modulate the Selective Toxicity of Polyene Macrolide Antifungals

  Publication

  • A. S. Skwarecki
  • K. Skarbek
  • D. Martynow
  • M. Serocki
  • I. Bylińska
  • M. J. Milewska
  • S. Milewski

  - BIOCONJUGATE CHEMISTRY - Year 2018

  Antifungal polyene macrolide antibiotics Amphotericin B (AmB) and Nystatin (NYS) were conjugated through the ω-amino acid linkers with diwalled “molecular umbrellas” composed of spermidine-linked deoxycholic or cholic acids. The presence of “umbrella” substituents modulated biological properties of the antibiotics, especially their selective toxicity. Some of the AmB-umbrella conjugates demonstrated antifungal in vitro activity...

  Full text to download in external service

Year 2017

• Synthesis and antimicrobial activity of 6-sulfo-6-deoxy-D-glucosamine and its derivatives

  Publication

  • K. Skarbek
  • I. Gabriel
  • P. Szweda
  • M. Wojciechowski
  • M. Khan
  • G. Boris
  • S. Milewski
  • M. J. Milewska

  - CARBOHYDRATE RESEARCH - Year 2017

  6-Sulfo-6-deoxy-D-glucosamine (GlcN6S), 6-sulfo-6-deoxy-D-glucosaminitol (ADGS) and their N-acetyl and methyl ester derivatives have been synthesized and tested as inhibitors of enzymes catalyzing reactions of the UDP-GlcNAc pathway in bacteria and yeasts. GlcN6S and ADGS at micromolar concentrations inhibited glucosamine-6-phosphate (GlcN6P) synthase of microbial origin. The former was also inhibitory towards fungal GlcN6P N-acetyl...

  Full text available to download

Year 2016

• Biosynthetic and synthetic access to amino sugars.

  Publication

  • K. Skarbek
  • M. J. Milewska

  - CARBOHYDRATE RESEARCH - Year 2016

  Amino sugars are important constituents of a number of biomacromolecules and products of mi crobial secondary metabolism, including antibiotics. For most of them, the amino group is located at the positions C1, C2 or C3 of the hexose or pentose ring. In biological systems, amino sugars are formed due to the catalytic activity of specific aminotransferases or amidotransferases by introducing an amino functionality derived from L-glutamate...

  Full text available to download

Year 2013

• Synthesis of 2-amino-2,6-dideoxy-D-glucitol-6-sulfonic acid as a potential antifungal agent.

  Publication

  • K. Skarbek

  - Year 2013

  Glucosamine-6P (GlcN-6P) synthase catalyzes the first committed step in the biosynthetic pathway leading to the formation of UDP-GlcNAc, a sugar nucleotide precursor providing D-glucosamine for the formation of chitin and manoproteins. 2-Amino-2,6-dideoxy-D-glucitol-6-sulfonic acid is an analog of 2-amino-2-deoxy-D-glucitol 6-phosphate (GlcN-ol-6-P), a known inhibitor of GlcN-6-P synthase, in which the phosphate group of the latter...

  Full text to download in external service