Article

MCH-R1 antagonists based on an arginine scaffold: SAR studies on the amino-terminus.

Procter & Gamble Pharmaceuticals, 8700 Mason-Montgomery Road, Mason, OH 45039, USA.
Bioorganic & Medicinal Chemistry Letters (impact factor: 2.55). 03/2007; 17(3):832-5. DOI:10.1016/j.bmcl.2006.10.056 pp.832-5
Source: PubMed

ABSTRACT We have identified a novel series of potent MCH-R1 antagonists based on l-arginine. As predicted by computational methods, there was an activity dependence on the pi-electronic character of the aromatic systems corresponding to the amino-terminus of these molecules. These results have enhanced our understanding of the MCH-R1 receptor and the potential for a predictive homology model.

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Keywords

activity dependence
 
aromatic systems corresponding
 
computational methods
 
novel series
 
pi-electronic character
 
potent MCH-R1 antagonists
 
predictive homology model
 

José Méndez-Andino