Synthesis and dopamine receptor modulating activity of unsubstituted and substituted triproline analogues of L-prolyl-L-leucyl-glycinamide (PLG)

Authors
Baures, PW Pradhan, A Ojala, WH Gleason, WB Mishra, RK Johnson, RL
Citation
Pw. Baures et al., Synthesis and dopamine receptor modulating activity of unsubstituted and substituted triproline analogues of L-prolyl-L-leucyl-glycinamide (PLG), BIOORG MED, 9(16), 1999, pp. 2349-2352
Citations number
23
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
16
Year of publication
1999
Pages
2349 - 2352
Database
ISI
SICI code
0960-894X(19990816)9:16<2349:SADRMA>2.0.ZU;2-H
Abstract
Triprolines Pro-Pro-Pro-NH2 (4), Pro-Pro-D-Pro-NH2 (5), Pro-Pro(trans-3-Me) -D-Pro-NH2 (6), and Pro-Pro(cis-3-Me)-D-Pro-NH2 (7) were made as conformati onally constrained analogues of Pro-Leu-Gly-NH2. Triprolines 4-6 produced s ignificant increases in the high- and low-affinity state ratio (R-H/R-L) of the dopamine receptor, but only 4 was found to increase apomorphine induce d rotations in 6-hydroxydopamine-lesioned rats. (C) 1999 Elsevier Science L td. All rights reserved.