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Synthesis of Tic-d-Phe Ψ[CH2–CH2] isostere and its use in the development of melanocortin receptor agonists
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Mar2006, Vol. 16 Issue 6, p1721-1725. 5p. - Publication Year :
- 2006
-
Abstract
- Abstract: The first synthesis of Tic-d-Phe Ψ[CH2–CH2] isostere is described, which features diastereoselective alkylation of the tricyclic lactam 14. The use of this novel dipeptide isostere in the development of melanocortin agonists has been demonstrated by the synthesis of peptidomimetic 7 and non-peptidic ligand 27. Both compounds displayed significant binding and agonist potency at the MC4R. [Copyright &y& Elsevier]
- Subjects :
- *PEPTIDE synthesis
*ALKYLATION
*CHEMICAL reactions
*LACTAMS
Subjects
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 16
- Issue :
- 6
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 19589905
- Full Text :
- https://doi.org/10.1016/j.bmcl.2005.12.005