Benzylpiperidine variations on histamine H 3 receptor ligands for improved drug-likeness

K Wingen, JS Schwed, K Isensee, L Weizel…

文献索引：Wingen, Kerstin; Schwed, J. Stephan; Isensee, Kathleen; Weizel, Lilia; Zivkovic, Aleksandra; Odazic, Dalibor; Stark, Holger Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 10 p. 2236 - 2239

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被引用次数: 2

摘要

Abstract Several hH 3 R antagonists/inverse agonists entered clinical phases for a broad spectrum of mainly centrally occurring diseases. Nevertheless, many promising candidates failed due to their pharmacokinetic profile, mostly because of their strong lipophilicity and their dibasic character. Analysis of previously, as potential PET ligands synthesized compounds (ST-889, ST-928) revealed promising results concerning physicochemical ...