Article

Novel carbazole derivatives as NPY Y1 antagonists.

GlaxoSmithKline Medicines Research Centre, Via A. Fleming 4, Verona 37135, Italy.
Bioorganic & Medicinal Chemistry Letters (impact factor: 2.55). 03/2007; 17(4):1043-6. DOI:10.1016/j.bmcl.2006.11.034 pp.1043-6
Source: PubMed

ABSTRACT The synthesis of a series of carbazole derivatives and their SAR at the NPY Y1 receptor is described. Modulation of physicochemical properties by appropriate decoration led to the identification of a high-affinity NPY Y1 antagonist that shows high brain penetration and modest oral bioavailability.

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Keywords

appropriate decoration
 
high-affinity NPY Y1 antagonist
 
modest oral bioavailability
 
Modulation
 
physicochemical properties