Structure-guided design and synthesis of position 1-phenylcycloalkylamine-derived pentapeptidic BACE1 inhibitors

…, Y Hamada, JT Nguyen, K Hidaka, T Hamada…

文献索引：Tagad, Harichandra D.; Hamada, Yoshio; Nguyen, Jeffrey-Tri; Hidaka, Koushi; Hamada, Takashi; Sohma, Youhei; Kimura, Tooru; Kiso, Yoshiaki Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 17 p. 5238 - 5246

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被引用次数: 12

摘要

Abstract Previously, we reported potent pentapeptidic BACE1 inhibitors with the hydroxymethylcarbonyl isostere as a substrate transition-state mimic. To improve the in vitro potency, we further reported pentapeptidic inhibitors with carboxylic acid bioisosteres at the P 4 and View the MathML source