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Wyniki wyszukiwania dla: immunosupresanty
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Estrowe koniugaty kwasu mykofenolowego i pochodnych akrydonów, estrowe koniugaty kwasu mykofenolowego i pochodnych akrydyn, sposób ich otrzymywania oraz zastosowanie jako immunosupresanty, zwłaszcza do stosowania w zapobieganiu odrzucaniu przeszczepów
WynalazkiKwas mykofenolowy (MPA) stosuje się w celu zapobiegania ostremu odrzuceniu przeszczepów nerek. Jako leki immunosupresyjne stosuje się nieestrowe i estrowe pochodne MPA, które powodują szereg efektów ubocznych, w tym biegunki, zwiększenie podatności na infekcje i nowotworzenie. Wciąż poszukuje się nowych leków o większej skuteczności leczenia i mniejszych efektach ubocznych. Znane jest wykorzystanie akrydyn...
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Synthesis and biological activity of ester derivatives of mycophenolic acid and acridines/acridones as potential immunosuppressive agents
PublikacjaImproved derivatives of mycophenolic acid (MPA) are necessary to reduce the frequency of adverse effects, this drug exerts in treated patients. In this study, MPA was coupled with N-(x-hydroxyalkyl)-9-acridone-4-carboxamides or N-(x-hydroxyalkyl)acridine-4-carboxamides to give respective ester conjugates upon Yamaguchi protocol. This esterification required protection of phenol group in MPA. Designed conjugates revealed higher...
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Approaches Towards Better Immunosuppressive Agents
PublikacjaSeveral classes of compounds are applied in clinics due to their immunosuppressive properties in transplantology and the treatment of autoimmune diseases. Derivatives of mycophe-nolic acid, corticosteroids and chemotherapeutics bearing heterocyclic moieties like methotrexate, azathioprine, mizoribine, and ruxolitinib are active substances with investigated mechanisms of action. However, improved synthetic approaches of known drugs...
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Synthesis and biological activity of mycophenolic acid-amino acid derivatives
PublikacjaIn search of new immunosuppressants, mycophenolic acid (MPA) was coupled with amino acid methyl esters followed by hydrolysis to analogs bearing free carboxylic groups. The obtained compunds were tested in vitro as growth inhibitors of lymphoid cell line (Jurkat) and human peripheral blood mononuclear cells (PBMC) from healthy donors. According to obtained results recovering of free carboxylic group increased their activity. Additionally,...
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Investigations on the immunosuppressive activity of derivatives of mycophenolic acid in immature dendritic cell
PublikacjaThe main activity of mycophenolic acid (MPA) and its analogs is the inhibition of proliferation of T cells. Here, we hypothesized that MPA and its conjugates inhibits also the activity of antigen-presenting cells (APC) including dendritic cells (DCs). We tested the effect of novel amino acid derivatives of MPA and conjugates of MPA with acridines/acridones on DCs by flow cytometry, ELISA and MLR assay. Both acridines/acridone derivatives...