期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 31, 期 6, 页码 974-982出版社
TAYLOR & FRANCIS LTD
DOI: 10.3109/14756366.2015.1077821
关键词
Acridines; acridones; esterification; IMPDH inhibitors; mycophenolic acid
资金
- National Centre for Research and Development (Poland) [LIDER/07/58/L-2/10/NCBiR/2011]
- Medical University of Gdansk [ST49]
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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