Design, synthesis, X-ray studies, and biological evaluation of novel BACE1 inhibitors with bicyclic isoxazoline carboxamides as the P3 ligand

We describe design, synthesis, X-ray studies, and biological evaluation of novel BACE1 inhibitors containing bicyclic isoxazoline carboxamides as the P3 ligand in combination with methyl cysteine, methylsulfonylalanine and Boc-amino alanine as P2 ligands. Inhibitor 3a displayed a BACE1 K(i) value of...

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Publicado no:Bioorg Med Chem Lett
Main Authors: Ghosh, Arun K., Ghosh, Koena, Brindisi, Margherita, Lendy, Emma K., Yen, Yu-Chen, Kumaragurubaran, Nagaswamy, Huang, Xiangping, Tang, Jordan, Mesecar, Andrew D.
Formato: Artigo
Idioma:Inglês
Publicado em: 2018
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6085084/
https://ncbi.nlm.nih.gov/pubmed/29970308
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2018.06.045
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