Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 31, Issue 6, Pages 974-982Publisher
TAYLOR & FRANCIS LTD
DOI: 10.3109/14756366.2015.1077821
Keywords
Acridines; acridones; esterification; IMPDH inhibitors; mycophenolic acid
Funding
- National Centre for Research and Development (Poland) [LIDER/07/58/L-2/10/NCBiR/2011]
- Medical University of Gdansk [ST49]
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Improved 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-(omega-hydroxyalkyl)-9-acridone-4-carboxamides or N-(omega-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 potency in vitro than parent MPA. Acridine derivatives were more active than acridone analogs and length of the alkyl linker between MPA and heterocyclic units influenced the observed cytotoxicity. Derivatives 2b, 2d, 3a, 3b displayed the most promising immunosuppressive activity.
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