Core refinement toward permeable β-secretase (BACE-1) inhibitors with low hERG activity

Journal of Medicinal Chemistry

Volumn 56, Issue 11, 2013, Pages 4181-4205

  Ginman, Tobias ^a   Viklund, Jenny ^a   Malmström, Jonas ^a   Blid, Jan ^a   Emond, Rikard ^a   Forsblom, Rickard ^a   Johansson, Anh ^a   Kers, Annika ^a   Lake, Fredrik ^a   Sehgelmeble, Fernando ^a   Sterky, Karin J ^a   Bergh, Margareta ^a   Lindgren, Anders ^a   Johansson, Patrik ^b   Jeppsson, Fredrik ^a   Fälting, Johanna ^a   Gravenfors, Ylva ^a   Rahm, Fredrik ^a  

^a ASTRAZENECA R AND D   (Sweden)

^b ASTRAZENECA R AND D   (Sweden)

Author keywords

[No Author keywords available]

Indexed keywords

2 (4 METHOXYPHENYL) 2 [3 (PYRIDIN 3 YL)PHENYL] 2,5 DIHYDROTHIAZOL 4 AMINE; 2 METHYL 2 [3 (PYRIMIDIN 5 YL)PHENYL] 5,6 DIHYDRO 2H 1,3 THIAZIN 4 AMINE; 4 (3' METHOXYBIPHENYL 3 YL) 4 METHYL 5,6 DIHYDRO 4H 1,3 THIAZIN 2 AMINE; 6 (4 METHOXYPHENYL) 2 METHYL 6 [3 (PYRIMIDIN 5 YL) PHENYL] 6H PYRROLO[3,4 D][1,3]THIAZOL 4 AMINE; AMIDINE; BETA SECRETASE 1 INHIBITOR; BETA SECRETASE INHIBITOR; POTASSIUM CHANNEL HERG; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BINDING SITE; CRYSTAL STRUCTURE; DRUG ACTIVITY; DRUG DESIGN; DRUG PENETRATION; DRUG SYNTHESIS; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; MOUSE; NONHUMAN; PHYSICAL CHEMISTRY; STRUCTURE ACTIVITY RELATION;

AMIDINES; AMYLOID PRECURSOR PROTEIN SECRETASES; ANIMALS; ASPARTIC ACID ENDOPEPTIDASES; BRAIN; CELL LINE, TUMOR; CELL MEMBRANE PERMEABILITY; CHO CELLS; COMPUTER SIMULATION; CRICETINAE; CRYSTALLOGRAPHY, X-RAY; DOGS; DRUG STABILITY; ETHER-A-GO-GO POTASSIUM CHANNELS; FEMALE; GUANIDINES; HUMANS; MADIN DARBY CANINE KIDNEY CELLS; MICE; MICE, INBRED C57BL; PROTEIN CONFORMATION; QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP; STEREOISOMERISM;

EID: 84879044939     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm3011349     Document Type: Article

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