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Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 22, 2010, Pages 6597-6605

Design and synthesis of aminohydantoins as potent and selective human β-secretase (BACE1) inhibitors with enhanced brain permeability

(15) Malamas, Michael S a Robichaud, Albert a,b Erdei, Jim a Quagliato, Dominick a Solvibile, William a Zhou, Ping a Morris, Koi a Turner, Jim a Wagner, Erik a Fan, Kristi a,c Olland, Andrea a Jacobsen, Steve a,d Reinhart, Peter a,d Riddell, David a Pangalos, Menelas a,e

a PFIZER INC (United States)

b LUNDBECK RESEARCH USA (United States)

c Vitae Pharmaceuticals (United States)

d Proteostasis Therapeutics (United States)

e ASTRAZENECA (United Kingdom)

Author keywords

Alzheimer's disease (AD); Aminohydantoins; BACE1 inhibitors; beta Amyloid peptide (A )

Indexed keywords

ALKYL GROUP; AMINOHYDANTOIN DERIVATIVE; AMYLOID BETA PROTEIN[1-40]; BETA SECRETASE 1; BETA SECRETASE INHIBITOR; CATHEPSIN D; CYTOCHROME P450 3A4; FLUORINE; HYDANTOIN DERIVATIVE; PEPSIN A; PHENYL GROUP; RENIN; SPHINGOLIPID ACTIVATOR PROTEIN 2; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; BRAIN PERMEABILITY; DRUG DESIGN; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; ENZYME INHIBITION; IN VIVO STUDY; METABOLISM; MOUSE; NONHUMAN; PERMEABILITY; PROTEIN BINDING; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION;

AMYLOID PRECURSOR PROTEIN SECRETASES; BRAIN; ENZYME INHIBITORS; HUMANS; HYDANTOINS; PERMEABILITY;

MUS;

EID: 77958038910 PISSN: 0960894X EISSN: None Source Type: Journal
DOI: 10.1016/j.bmcl.2010.09.029 Document Type: Article

Times cited : (50)

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