AI Article Synopsis
- The article discusses the development of benzhydrol derivatives that are powerful inhibitors of squalene synthase but failed to show adequate effectiveness for clinical use.
- The research then shifted towards creating a more effective compound by utilizing a benzoxazepine structure.
- The newly designed pyrrolobenzoxazepine derivatives demonstrated improved in vitro and in vivo activity compared to the initial compounds.
Article 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 new tricyclic scaffold by the incorporation of heterocycle into it. Prepared pyrrolobenzoxazepine derivatives showed further efficient in vitro and in vivo activities.
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| http://dx.doi.org/10.1016/j.bmc.2012.02.054 | DOI Listing |
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