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Discovery of novel tricyclic compounds as squalene synthase inhibitors

M Ichikawa, M Ohtsuka, H Ohki, N Haginoya…

文献索引:Ichikawa, Masanori; Ohtsuka, Masami; Ohki, Hitoshi; Haginoya, Noriyasu; Itoh, Masao; Sugita, Kazuyuki; Usui, Hiroyuki; Suzuki, Makoto; Terayama, Koji; Kanda, Akira Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 9 p. 3072 - 3093

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被引用次数: 10

摘要

In the present article, we have reported the design, synthesis, and identification of highly potent benzhydrol derivatives as squalene synthase inhibitors (compound 1). Unfortunately, the in vivo efficacies of the compounds were not enough for acquiring the clinical candidate. We continued our investigation to obtain a more in vivo efficacious template than the benzhydrol template. In our effort, we focused on a benzoxazepine ring and designed a ...