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Pyrrolidines as potent functional agonists of the human melanocortin-4 receptor.

Authors :
Tran JA
Chen CW
Jiang W
Tucci FC
Fleck BA
Marinkovic D
Arellano M
Chen C
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Sep 15; Vol. 17 (18), pp. 5165-70. Date of Electronic Publication: 2007 Jul 04.
Publication Year :
2007

Abstract

A series of pyrrolidine derivatives were synthesized and characterized as potent agonists of the human melanocortin-4 receptor. For example, 28c had a K(i) of 13 nM in binding affinity and EC(50) of 6.9 nM in agonist potency with an intrinsic activity of 100% of the endogenous ligand alpha-MSH.

Details

Language :
English
ISSN :
0960-894X
Volume :
17
Issue :
18
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
17629702
Full Text :
https://doi.org/10.1016/j.bmcl.2007.06.088