| Autor: |
Chen L; Center for Drug Design, Academic Health Center, University of Minnesota, 516 Delaware Street S.E., Minneapolis, MN 55455, USA. chenx462@umn.edu, Wilson DJ, Labello NP, Jayaram HN, Pankiewicz KW |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2008 Oct 15; Vol. 16 (20), pp. 9340-5. Date of Electronic Publication: 2008 Aug 29. |
| DOI: |
10.1016/j.bmc.2008.08.062 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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