双环杂环作为强效 γ-分泌酶调节剂的设计与合成。
Design and synthesis of bicyclic heterocycles as potent γ-secretase modulators.
机构信息
Neuroscience, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium.
出版信息
Bioorg Med Chem Lett. 2013 Sep 1;23(17):4794-800. doi: 10.1016/j.bmcl.2013.06.100. Epub 2013 Jul 11.
PMID:23890837
Abstract
The evolution of amide 3 into conformationally restricted bicyclic triazolo-piperidine 14-S as a γ-secretase modulator is described. This is a potential disease modifying anti-Alzheimer's drug which demonstrated high in vitro and in vivo potency against Aβ42 peptide, reduced lipophilicity and enhanced brain free fraction compared to the previous series.
摘要
酰胺 3 演变为构象受限的双环三唑并哌啶 14-S 作为 γ-分泌酶调节剂的过程被描述。这是一种有潜力的治疗阿尔茨海默病的药物，与前一系列化合物相比，它对 Aβ42 肽具有高体外和体内活性，降低了亲脂性，并提高了脑游离分数。
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