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Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors |
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| Authors: | Ying-zi Xu Shendong Yuan Simeon Bowers Roy K Hom Wayman Chan Hing L Sham Yong L Zhu Paul Beroza Hu Pan Eric Brecht Nanhua Yao Julie Lougheed Jiangli Yan Danny Tam Zhao Ren Lany Ruslim Michael P Bova Dean R Artis |
| Institution: | 1. Department of Chemical Sciences, Elan Pharmaceuticals, 180 Oyster Point Boulevard, South San Francisco, CA 94080, USA;2. Department of Molecular Design, Elan Pharmaceuticals, 180 Oyster Point Boulevard, South San Francisco, CA 94080, USA |
| Abstract: | Utilizing a structure based design approach, combined with extensive medicinal chemistry execution, highly selective, potent and novel BACE1 inhibitor 8 (BACE1 Alpha assay IC50 = 8 nM) was made from a weak μM potency hit in an extremely efficient way. The detailed SAR and general design approaches will be discussed. |
| Keywords: | BACE1 inhibitor Structural based drug design SAR Selectivity |
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