1.
Bioorg Med Chem Lett
; 17(4): 1043-6, 2007 Feb 15.
Article
in English
| MEDLINE
| ID: mdl-17127055
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.
Subject(s)
Carbazoles/chemical synthesis , Carbazoles/pharmacology , Receptors, Neuropeptide Y/antagonists & inhibitors , Animals , Biological Availability , Brain/drug effects , Brain/metabolism , CHO Cells , Carbazoles/pharmacokinetics , Chemical Phenomena , Chemistry, Physical , Cricetinae , Cricetulus , Half-Life , Indicators and Reagents , Male , Rats , Rats, Sprague-Dawley , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 16(6): 1749-52, 2006 Mar 15.
Article
in English
| MEDLINE
| ID: mdl-16364642
ABSTRACT
The SAR of a new series of tetrahydrocarbazole derivatives is described: the appropriate decoration of this template led to the identification of a new class of NPY-1 antagonists showing good in vitro potency and a promising in vivo pharmacokinetic profile in rat.
