Urotensin-II receptor antagonists: Synthesis and SAR of N-cyclic azaalkyl benzamides
SAR exploration of the central diamine, benzyl, and terminal aminoalkoxy regions of the N-cyclic azaalkyl benzamide series led to the identification of very potent human urotensin-II receptor antagonists such as 1a with a Ki of 4 nM. The synthesis and structure-activity relationships (SAR) of N-cyclic azaalkyl benzamides are described.
Jin, Jian,An, Ming,Sapienza, Anthony,Aiyar, Nambi,Naselsky, Diane,Sarau, Henry M.,Foley, James J.,Salyers, Kevin L.,Knight, Steven D.,Keenan, Richard M.,Rivero, Ralph A.,Dhanak, Dashyant,Douglas, Stephen A.
scheme or table
p. 3950 - 3954
(2009/05/07)
Urotensin-II receptor antagonists
The present invention relates to pyrrolyl and pyridyl derivatives, pharmaceutical compositions containing them and their use as inhibitors of urotensin II.