| Literature DB >> 20042333 |
Derek C Cole1, Jonathan L Gross, Thomas A Comery, Suzan Aschmies, Warren D Hirst, Cody Kelley, Ji-In Kim, Katie Kubek, Xiaoping Ning, Brian J Platt, Albert J Robichaud, William R Solvibile, Joseph R Stock, Gregory Tawa, Marla J Williams, John W Ellingboe.
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. Copyright (c) 2009 Elsevier Ltd. All rights reserved.Entities:
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Year: 2009 PMID： 20042333 DOI： 10.1016/j.bmcl.2009.11.122
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823