Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints - Winneroski, Leonard L.; Erickson, Jon A.; Green, Steven J.; Lopez, Jose E.; Stout, Stephanie L.; Porter, Warren J.; Timm, David E.; Audia, James E.; Barberis, Mario; Beck, James P.; Boggs, Leonard N.; Borders, Anthony R.; et al. (Bioorganic & medicinal chemistry, 2020)
Keywords: Alzheimer Disease - drug therapy; Alzheimer Disease - metabolism; Alzheimer’s disease; Amyloid Precursor Protein Secretases - antagonists & inhibitors; Amyloid Precursor Protein Secretases - metabolism; Aspartic Acid Endopeptidases - antagonists & inhibitors; Aspartic Acid Endopeptidases - metabolism; BACE1 inhibitor; Biochemistry & Molecular Biology; Chemistry; Chemistry, Medicinal; Chemistry, Organic; Conformational constraint; Crystallography, X-Ray; Cyclopropanes - chemical synthesis; Cyclopropanes - chemistry; Cyclopropanes - pharmacology; Cyclopropyl; Dose-Response Relationship, Drug; Humans; Life Sciences & Biomedicine; Ligands; Models, Molecular; Molecular Conformation; Pharmacology & Pharmacy; Physical Sciences; Protease Inhibitors - chemical synthesis; Protease Inhibitors - chemistry; Protease Inhibitors - pharmacology; Science & Technology; Structure-Activity Relationship; Structure-based drug design; Cyclopropyl; BACE1 inhibitor; Conformational constraint; Structure-based drug design; Alzheimer’s disease; BETA-SECRETASE; AMYLOID-BETA; MICE; Alzheimer's disease