About: Preparation of Peptidomimetic Prodrugs of Acyclic Nucleoside Phosphonates as Antivirals with Improved Bioavailability     Goto   Sponge   NotDistinct   Permalink

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  • Transformation of acyclic nucleoside phosphonates (ANPs) to appropriate prodrugs helps to improve their low bioavailability connected with a limited transport through the cell membrane caused by a presence of negative charges in the molecule. The advantage of peptidomimetic prodrugs is releasing of an active compound in target tissue together with a completely nontoxic and natural accompanying material as by-product. Development of orally active peptide drugs is often limited by their unfavorable physicochemical properties. However, their appropriate structural modifications to form peptidomimetics, especially modifications increasing the hyhobicity but simultaneously decreasing the hydrogen bonding potential open the way to circumvent metabolic enzymes and improve their oral bioavailability. In the field of ANPs we will focus to strategy originally developed in McKenna’s group based on esterification of ANPs with a side-chain hydroxyl group of some serine containing dipeptides. (en)
  • Cílem projektu je syntéza nového typu netoxických profarmak acyklických nukleosidfosfonátů s modifikovaným dipeptidovým zbytkem a na základě studia jejich farmakokinetických vlastností výběr kandidátů pro potenciální vývoj budoucího léčiva.
Title
  • Preparation of Peptidomimetic Prodrugs of Acyclic Nucleoside Phosphonates as Antivirals with Improved Bioavailability (en)
  • Příprava peptidomimetických profarmak acyklických nukleosidfosfonátů jako antivirotik se zvýšenou biologickou využitelností
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  • ME10040
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  • Phosphonates Acyclic nucleoside phosphonates ANP Nucleotides Nucleotide analogs Antivirals Prodrugs Bioavailability Peptidomimetics (en)
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  • New synthetic methodology leading to dipeptide and amino acid prodrugs of various acyclic nucleoside phosphonates has been worked out and the samples tested for antiviral activity. For further development, tyrosine esters and long chain alkylated tyrosine amide derivatives were found the most optimal from a pharmacological view point due to a high plasma stability and good bioavailability. (en)
  • Byla vypracována metodika syntézy dipeptidických a aminokyselinových profarmak různých typů acyklických nukleosidfosfonátů a vzorky testovány na protivirovou aktivitu. Tyrosinové estery a tyrosinamidové deriváty alkylované dlouhými mastnými řetězci byly z farmakologického hlediska shledány jako nejoptimálnější pro další vývoj vzhledem k vysoké stabilitě v plasmě a dobré biodostupnosti. (cs)
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