title: Design and synthesis of BACE-1 inhibitors utilizing a tertiary hydroxyl motif as the transition state mimic.
abstract: Two series of drug-like BACE-1 inhibitors with a shielded tertiary hydroxyl as transition state isostere have been synthesized. The most potent inhibitor exhibited a BACE-1 IC(50) value of 0.23 microM.
authors: Organic Pharmaceutical Chemistry, Department of Medicinal Chemistry, Uppsala University, BMC, SE-751 23 Uppsala, Sweden.
authors: Fredrik
authors: F
authors: Wångsell
authors: Francesco
authors: F
authors: Russo
authors: Jonas
authors: J
authors: Sävmarker
authors: Asa
authors: A
authors: Rosenquist
authors: Bertil
authors: B
authors: Samuelsson
authors: Mats
authors: M
authors: Larhed
mesh_terms: D000596:Amino Acids / Q000737:chemistry; D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D016282:Aspartic Acid Endopeptidases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D002402:Cathepsin D / Q000378:metabolism; D015195:Drug Design; D006801:Humans; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000596:Amino Acids; D011480:Protease Inhibitors; D053829:Amyloid Precursor Protein Secretases; D016282:Aspartic Acid Endopeptidases; C509280:BACE1 protein, human; D002402:Cathepsin D; C013165:statine