|
|||||
|
|
Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors |
|
| Authors: | Thompson Lorin A Liauw Ann Y Ramanjulu Mercy M Kasireddy-Polam Padmaja Mercer Stephen E Maduskuie Thomas P Glicksman Marcie Roach Arthur H Meredith Jere E Liu Rui-Qin Combs Andrew P Higaki Jeffrey N Cordell Barbara Seiffert Dietmar Zaczek Robert C Robertson David W Olson Richard E |
| Institution: | Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. lorin.thompson@bms.com |
| Abstract: | The synthesis, evaluation, and structure-activity relationships of a series of succinoyl lactam inhibitors of the Alzheimer's disease gamma-secretase are described. Beginning with a screening hit with broad proteinase activity, optimization provided compounds with both high selectivity for inhibition of gamma-secretase and high potency in cellular assays of A beta reduction. The SAR and early in vivo properties of this series of inhibitors will be presented. |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |