| Autor: |
Hudack RA Jr; Department of Chemistry, Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA., Barta NS, Guo C, Deal J, Dong L, Fay LK, Caprathe B, Chatterjee A, Vanderpool D, Bigge C, Showalter R, Bender S, Augelli-Szafran CE, Lunney E, Hou X |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2006 Feb 09; Vol. 49 (3), pp. 1202-6. |
| DOI: |
10.1021/jm049161u |
| Abstrakt: |
Since the discovery that FK-506 promotes neurite outgrowth, considerable attention has been focused on the development of potent nonimmunosuppressive ligands for FK-506 binding proteins (FKBPs). Such neuroimmunophilin agents have been reported to show neuroregenerative activity in a variety of cell and animal models including neurite outgrowth, age-related cognitive decline, Parkinson's disease, peripheral nerve injury, optic nerve degeneration, and diabetic neuropathy. We have designed and synthesized a unique series of tetracyclic aza-amides that have been shown to be potent FKBP12 rotamase inhibitors. The structure-activity relationships established in this study have demonstrated diverse structural modifications that result in potent rotamase inhibitory activity. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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