Details

Autor(en) / Beteiligte

• Xu, Ruo
• Cole, David
• Asberom, Ted
• Bara, Tom
• Bennett, Chad
• Burnett, Duane A.
• Clader, John
• Domalski, Martin
• Greenlee, William J.
• Hyde, Lynn
• Josien, Hubert
• Li, HongMei
• McBriar, Mark
• McKittrick, Brian
• Pissarnitski, Dmitri
• Qiang, Li
• Rajagopalan, Murali
• Sasikumar, Thavalakulamgara
• Su, Jing
• Tang, HaiQun
• Wu, Wen-Lian
• Zhang, LiLi
• Zhao, ZhiQiang

Titel

SAR of tricyclic sulfones as γ-secretase inhibitors

Ist Teil von

• Science China. Chemistry, 2011-11, Vol.54 (11), p.1688-1701

Ort / Verlag

Heidelberg: SP Science China Press

Erscheinungsjahr

2011

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• Novel tricyclic sulfones as γ-secretase inhibitors have been reported by this laboratory for the treatment of Alzheimer＇s disease Compounds in this series have comparable or better in vitro activities and in vivo efficacies than sulfonamide analogues re- ported previously by this laboratory. Based on the previously reported tricyclic sulfone scaffold, additional SAR studies of C ring were carried out. Various C-ring structures including cyclohexane, pyran, and piperidine were tolerated. Additionally, the 7- and 8- positions of the C-ring were identified as the best sites to introduce substituent for modulating the pharmacokinetic properties of compounds from this series.