Discovery of novel tricyclic compounds as squalene synthase inhibitors

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

Index: 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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Citation Number: 10

Abstract

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 ...