Prolonged stability by cyclization: Macrocyclic phosphino dipeptide isostere inhibitors of β-secretase (BACE1)

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 15, 2009, Pages 4427-4431

  Huber, Timo ^a   Manzenrieder, Florian ^a   Kuttruff, Christian A ^a   Dorner Ciossek, Cornelia ^b   Kessler, Horst ^a  

^a Munich Center for Integrated Protein Science   (Germany)

^b BOEHRINGER INGELHEIM PHARMA GMBH AND CO KG   (Germany)

Author keywords

Secretase; Alzheimer's disease; BACE1; Macrocyclic; Phosphino dipeptide isostere; Serum stability

Indexed keywords

ALKENE; BETA SECRETASE INHIBITOR; MACROCYCLIC INHIBITOR; PSEUDO PEPTIDIC INHIBITOR DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; CYCLIZATION; DRUG STRUCTURE; HALF LIFE TIME; HUMAN; IC 50; SERUM;

ALZHEIMER DISEASE; AMYLOID PRECURSOR PROTEIN SECRETASES; ANIMALS; ASPARTIC ACID ENDOPEPTIDASES; CHEMISTRY, PHARMACEUTICAL; DIPEPTIDES; DRUG DESIGN; HUMANS; INHIBITORY CONCENTRATION 50; MICE; MICE, KNOCKOUT; MODELS, BIOLOGICAL; MODELS, CHEMICAL; MODELS, MOLECULAR; MOLECULAR CONFORMATION; PEPTIDES; PHENOTYPE; TIME FACTORS;

EID: 67649981158     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.05.053     Document Type: Article

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