Aminoalkoxybenzyl pyrrolidines as novel human urotensin-II receptor antagonists
4区 · 医学
Article
作者: Dulcie B. Schmidt ; Gregory L. Warren ; Carl D. Bennett ; James J. Foley ; Dashyant Dhanak ; Michael L. Moore ; Jian Jin ; Henry M. Sarau ; Diane Naselsky ; Katherine Widdowson ; Stephen A. Douglas ; Ralph A. Rivero ; Richard M. Keenan ; Steven D. Knight ; Bing Wang ; Nambi Aiyar
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.