期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 15, 页码 4115-4118出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.06.008
关键词
Azetidine carboxylic acids; 3,4-Didehydro-(S)-proline; Didehydro-alanine; Endomorphins; mu-Receptors
资金
- U. S. Public Health Service, National Institute of Drug Abuse [DA06284, DA13449]
Six new endomorphin analogues, incorporating constrained amino acids in place of native proline have been synthesized. Residues of (S)-azetidine-2-carboxylic acid (Aze), 3,4-dehydro-(S)-proline (Delta(3)Pro), azetidine-3-carboxylic acid (3Aze) and dehydro-alanine (Delta Ala) have been used to prepare [Delta(3)Pro(2)]EM-2 (1), [Aze(2)]EM-1 (2), [Aze(2)]EM-2 (3), [3Aze(2)]EM-1 (4), [3Aze(2)]EM-2 (5) and [Delta Ala(2)]EM-2 (6). Binding assays and functional bioactivities for mu-and delta-receptors are reported. The highest affinity, bioactivity and selectivity are shown by peptides 2 and 3 containing the Aze residue. (C) 2009 Elsevier Ltd. All rights reserved.
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