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Bioorg Med Chem Lett. 2010 Feb 1;20(3):1237-40. doi: 10.1016/j.bmcl.2009.11.122. Epub 2009 Dec 4.

Benzimidazole- and indole-substituted 1,3'-bipyrrolidine benzamides as histamine H3 receptor antagonists.

Author information

1
Chemical Sciences, Wyeth Research, 401 N Middletown Rd. Pearl River, NY 10965, United States. coledc@wyeth.com

Abstract

Using a focused screen of biogenic amine compounds we identified a novel series of H(3)R antagonists. A preliminary SAR study led to reduction of MW while increasing binding affinity and potency. Optimization of the physical properties of the series led to (S)-6n, with improved brain to plasma exposure and efficacy in both water intake and novel object recognition models.

PMID:
20042333
DOI:
10.1016/j.bmcl.2009.11.122
[Indexed for MEDLINE]

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