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1篇 您的检索式:作者名="DOMALSKI Martin"
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1SAR of tricyclic sulfones as γ-secretase inhibitors显示文摘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.COLE David ASBEROM Ted BARA Tom BENNETT Chad BURNETT Duane A. CLADER John DOMALSKI Martin GREENLEE William J. HYDE Lynn JOSIEN Hubert McBRIAR Mark McKITTRICK Brian PISSARNITSKI Dmitri RAJAGOPALAN Murali SASIKUMAR Thavalakulamgara 2011Science China Chemistry2011,54,11:0
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