Referenced in: none

Automatically associated channels: Kv11.1

Title: The discovery of fused oxadiazepines as gamma secretase modulators for treatment of Alzheimer's disease.

Authors: Hongmei Li, Jun Qin, Pawan Dhondi, Wei Zhou, Monica Vicarel, Thomas Bara, David Cole, Hubert Josien, Dmitri Pissarnitski, Zhaoning Zhu, Anandan Palani, Robert Aslanian, John Clader, Michael Czarniecki, William Greenlee, Mary Cohen-Williams, Lynn Hyde, Lixin Song, Lili Zhang, Inhou Chu, Xianhai Huang

Journal, date & volume: Bioorg. Med. Chem. Lett., 2013 Jan 15 , 23, 466-71

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/23253441

Abstract
In an attempt to further improve overall profiles of the oxadiazine series of GSMs, in particular the hERG activity, conformational modifications of the core structure resulted in the identification of fused oxadiazepines such as 7i which had an improved hERG inhibition profile and was a highly efficacious GSM in vitro and in vivo in rats. These SAR explorations offer opportunities to identify potential drugs to treat Alzheimer's disease.