The design of dipeptide helical mimetics: the synthesis and biological activity of trisubstituted indanes
| Autor: | Henriëtte M. G. Willems, William Howson, David Christopher Horwell, Ratcliffe Giles S |
|---|---|
| Rok vydání: | 1994 |
| Předmět: |
chemistry.chemical_classification
Dipeptide Chemistry Stereochemistry Organic Chemistry Clinical Biochemistry Pharmaceutical Science Biological activity Biochemistry Combinatorial chemistry Amino acid chemistry.chemical_compound Drug Discovery Molecular Medicine Tachykinin receptor Molecular Biology |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 4:2825-2830 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(01)80821-0 |
| Popis: | The design and synthesis of conformationally constrained, non-peptide templates (trisubstituted indanes) which allow the incorporation of two adjacent amino acid side-chains plus a third binding group in an orientation similar to that found in alpha-helices is reported. The tachykinin receptor affinity of various Phe-Phe and Trp-Phe mimetics were detemined and several were shown to bind with micromolar affinity. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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