کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10582652 | 981075 | 2012 | 22 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of novel tricyclic compounds as squalene synthase inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
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 new tricyclic scaffold by the incorporation of heterocycle into it. Prepared pyrrolobenzoxazepine derivatives showed further efficient in vitro and in vivo activities.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 9, 1 May 2012, Pages 3072-3093
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 9, 1 May 2012, Pages 3072-3093
نویسندگان
Masanori Ichikawa, Masami Ohtsuka, Hitoshi Ohki, Noriyasu Haginoya, Masao Itoh, Kazuyuki Sugita, Hiroyuki Usui, Makoto Suzuki, Koji Terayama, Akira Kanda,