Design, Synthesis, and Biological Activity of Novel Polycyclic Aza-Amide FKBP12 Ligands
| العنوان: | Design, Synthesis, and Biological Activity of Novel Polycyclic Aza-Amide FKBP12 Ligands |
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| المؤلفون: | Dong Liming, Xinjun Hou, Elizabeth A. Lunney, Corinne E. Augelli-Szafran, Deal Judith G, Christopher F. Bigge, Darin Vanderpool, Raymond Andrew Hudack, Nancy Sue Barta, Bradley William Caprathe, Chuangxing Guo, Steve Bender, Richard E. Showalter, Lorraine Kathleen Fay, Arindam Chatterjee |
| المصدر: | Journal of Medicinal Chemistry. 49:1202-1206 |
| بيانات النشر: | American Chemical Society (ACS), 2006. |
| سنة النشر: | 2006 |
| مصطلحات موضوعية: | Peptidylprolyl isomerase, Aza Compounds, Binding Sites, Neurite, Chemistry, Hydrogen Bonding, Biological activity, Tacrolimus Binding Protein 1A, Isoquinolines, Ligands, Amides, Heterocyclic Compounds, 4 or More Rings, Tacrolimus, Structure-Activity Relationship, Neuroprotective Agents, FKBP, Biochemistry, Cis-trans-Isomerases, Drug Discovery, Molecular Medicine, Structure–activity relationship, Binding site, Cognitive decline |
| الوصف: | 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. |
| تدمد: | 1520-4804 0022-2623 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::91fb4d75bb6365379c9f5766e6a1b084 https://doi.org/10.1021/jm049161u |
| رقم الأكسشن: | edsair.doi.dedup.....91fb4d75bb6365379c9f5766e6a1b084 |
| قاعدة البيانات: | OpenAIRE |
Find this issue from the American Chemical Society | تدمد: | 15204804 00222623 |
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