Carbazole-containing arylcarboxamides as BACE1 inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 22, 2011, Pages 6657-6661

  Bertini, Simone ^a   Asso, Valentina ^a   Ghilardi, Elisa ^a   Granchi, Carlotta ^a   Manera, Clementina ^a   Minutolo, Filippo ^a   Saccomanni, Giuseppe ^a   Bortolato, Andrea ^b   Mason, Jonathan ^b,d   Moro, Stefano ^c   MacChia, Marco ^a  

^a UNIVERSITY OF PISA   (Italy)

^b Heptares Therapeutics Ltd   (United Kingdom)

^c UNIVERSITY OF PADOVA   (Italy)

^d H LUNDBECK A S   (Denmark)

Author keywords

Alzheimer; BACE1; Carbazole; Flap; Molecular docking

Indexed keywords

ALPHA NAPHTHYLAMINOPROPAN 2 OL CARBAZOLE; BETA SECRETASE 1; BETA SECRETASE INHIBITOR; CARBAZOLE DERIVATIVE; CYTOCHROME P450 2C9; CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; ISOLEUCINE; N [3 (9H CARBAZOL 9 YL) 2 HYDROXYPROPYL]ARYLCARBOXAMIDE; THREONINE; TYROSINE; UNCLASSIFIED DRUG; VALINE;

ACYLATION; ARTICLE; BLOOD BRAIN BARRIER; CRYSTAL STRUCTURE; DRUG PENETRATION; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; INTESTINE ABSORPTION; MOLECULAR DOCKING; PLASMA PROTEIN BINDING; PREDICTION; STRUCTURE ACTIVITY RELATION;

ALZHEIMER DISEASE; AMIDES; AMYLOID PRECURSOR PROTEIN SECRETASES; ASPARTIC ACID ENDOPEPTIDASES; BLOOD-BRAIN BARRIER; CARBAZOLES; ENZYME INHIBITORS; HUMANS; MODELS, MOLECULAR; PROTEIN BINDING; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 80054733253     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.09.064     Document Type: Article

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