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.
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Aminoalkoxybenzyl pyrrolidines as novel human urotensin-II receptor antagonists.
Bioorg Med Chem Lett
July 2005
High Throughput Chemistry, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA.
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.
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