N-Phenylphenylglycines as Novel Corticotropin Releasing Factor Receptor Antagonists
Screening of a computationally designed synthetic library led to the discovery of the N-phenylphenylglycines (NPPGs) as a novel class of human corticotropin releasing factor (h-CRF1) antagonists. Several NPPGs with greater potency than the original hit 1 were rapidly identified, and resolution of the racemate demonstrated that only the R-enantiomer displays activity. This structural class represents the first example of a non-peptide CRF1 antagonist with a stereochemically distinct receptor binding affinity.
Molteni, Valentina,Penzotti, Julie,Wilson, Dean M.,Termin, Andreas P.,Mao, Long,Crane, Christine M.,Hassman, Fred,Wang, Tao,Wong, Harvey,Miller, Keith J.,Grossman, Scott,Grootenhuis, Peter D. J.
p. 2426 - 2429
(2007/10/03)
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