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

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.

DOI: 10.1016/j.bmcl.2009.11.122

Cite this paper

@article{Cole2010BenzimidazoleAI, title={Benzimidazole- and indole-substituted 1,3'-bipyrrolidine benzamides as histamine H3 receptor antagonists.}, author={Derek C Cole and Jonathan L. Gross and Thomas A. Comery and Suzan H Aschmies and Warren D. Hirst and Cody Kelley and Ji-In Kim and Katie Kubek and Xiaoping Ning and Brian J. Platt and Albert J. Robichaud and William R Solvibile and Joseph R. Stock and Gregory J. Tawa and Marla J Williams and John W Ellingboe}, journal={Bioorganic & medicinal chemistry letters}, year={2010}, volume={20 3}, pages={1237-40} }