Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 16, Issue 20, Pages 9340-9345Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.08.062
Keywords
mycophenolic acid; inosine monophosphate dehydrogenase; allylic substitution
Funding
- Center for Drug Design, Academic Health Center, University of Minnesota
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Mycophenolic acid (MPA), a clinically used immunosuppressant, is extensively metabolized into an inactive C7-glucuronide and removed from circulation. To circumvent the metabolic liability imposed by the C7-hydroxyl group, we have designed a series of hybrid MPA analogs based on the pharmacophores present in MPA and new generations of inosine monophosphate dehydrogenase (IMPDH) inhibitors. The synthesis of MPA analogs has been accomplished by an allylic substitution of a common lactone. Biological evaluations of these analogs and a preliminary structure-activity relationship (SAR) are presented. (c) 2008 Elsevier Ltd. All rights reserved.
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