852324-85-7Relevant articles and documents
Urotensin-II receptor antagonists: Synthesis and SAR of N-cyclic azaalkyl benzamides
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)
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.
NOVEL M3 MUSCARINIC ACETYCHOLINE RECEPTOR ANTAGONISTS
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Page/Page column 27, (2008/06/13)
Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.
Aminoalkoxybenzyl pyrrolidines as novel human urotensin-II receptor antagonists
Jin, Jian,Dhanak, Dashyant,Knight, Steven D.,Widdowson, Katherine,Aiyar, Nambi,Naselsky, Diane,Sarau, Henry M.,Foley, James J.,Schmidt, Dulcie B.,Bennett, Carl D.,Wang, Bing,Warren, Gregory L.,Moore, Michael L.,Keenan, Richard M.,Rivero, Ralph A.,Douglas, Stephen A.
, p. 3229 - 3232 (2007/10/03)
High throughput screening of the corporate compound collection led to the discovery of a novel series of substituted aminoalkoxybenzyl pyrrolidines as human urotensin-II receptor antagonists. The synthesis, initial structure-activity relationships, and optimization of the initial hit that led to the identification of a truncated sub-series, represented by SB-436811 (1a), are described.
