Aminoalkoxybenzyl pyrrolidines as novel human urotensin-II receptor antagonists

  • Bioorg Med Chem Lett. 2005 Jul 1;15(13):3229-32. doi: 10.1016/j.bmcl.2005.04.074.
Jian Jin  1 ,  Dashyant Dhanak ,  Steven D Knight ,  Katherine Widdowson ,  Nambi Aiyar ,  Diane Naselsky ,  Henry M Sarau ,  James J Foley ,  Dulcie B Schmidt ,  Carl D Bennett ,  Bing Wang ,  Gregory L Warren ,  Michael L Moore ,  Richard M Keenan ,  Ralph A Rivero ,  Stephen A Douglas
Affiliations
  • 1. High Throughput Chemistry, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA. [email protected]
PMID: 15936190 DOI: 10.1016/j.bmcl.2005.04.074
Abstract

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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