2. Academic Validation
  3. Aminoalkoxybenzyl pyrrolidines as novel human urotensin-II receptor antagonists

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

Affiliation

  • 1 High Throughput Chemistry, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA. jian.jin@gsk.com
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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