Bicyclic Tripeptide Mimetics with Reverse Turn Inducing Properties
| العنوان: | Bicyclic Tripeptide Mimetics with Reverse Turn Inducing Properties |
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| المؤلفون: | and Anders Karlén, Anders Hallberg, Gunnar Lindeberg, Weimin Tong, Petra Johannesson, Adolf Gogoll |
| المصدر: | Journal of Medicinal Chemistry. 42:601-608 |
| بيانات النشر: | American Chemical Society (ACS), 1999. |
| سنة النشر: | 1999 |
| مصطلحات موضوعية: | Models, Molecular, Magnetic Resonance Spectroscopy, Stereochemistry, Thiazolidine, Peptide, CHO Cells, Tripeptide, In Vitro Techniques, Receptor, Angiotensin, Type 2, Protein Structure, Secondary, Receptor, Angiotensin, Type 1, Turn (biochemistry), Radioligand Assay, chemistry.chemical_compound, Cricetinae, Drug Discovery, Peptide synthesis, Animals, Vasoconstrictor Agents, chemistry.chemical_classification, Receptors, Angiotensin, Angiotensin II receptor type 1, Bicyclic molecule, Angiotensin II, Molecular Mimicry, Rats, Liver, chemistry, Molecular Medicine |
| الوصف: | Analogues of the hypertensive octapeptide angiotensin II, comprising novel constrained 5,8-bicyclic and 5,9-bicyclic tripeptide units adopting nonclassical beta-turn geometries, as deduced from theoretical conformational analysis, have been synthesized. Spontanous bicyclization upon acid-catalyzed deprotection of a model peptide, encompassing a protected omega-formyl alpha-amino acid in position 5 and cysteine residues in positions 3 and 7, revealed a strong preference for bicyclization toward the C-terminus. The bicyclic thiazolidine related angiotensin II analogues synthesized exhibited no affinity for the angiotensin II AT1 receptor. |
| تدمد: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm981077p |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::79830fb30d2dcfe995095eb2026f9422 https://doi.org/10.1021/jm981077p |
| رقم الانضمام: | edsair.doi.dedup.....79830fb30d2dcfe995095eb2026f9422 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 15204804 00222623 |
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| DOI: | 10.1021/jm981077p |