Design and synthesis of 1,4-dihydropyridine derivatives as BACE-1 inhibitors

European Journal of Medicinal Chemistry

Volumn 45, Issue 6, 2010, Pages 2578-2590

  Choi, Soo Jeong ^a   Cho, Joong Heui ^a   Im, Isak ^a   Lee, So Deok ^a   Jang, Ji Yeon ^b   Oh, Yu Min ^b   Jung, Yong Keun ^b   Jeon, Eun Seok ^c   Kim, Yong Chul ^a  

^a Gwangju Institute of Science and Technology (GIST)   (South Korea)

^b Seoul National University   (South Korea)

^c Sungkyunkwan University School of Medicine   (South Korea)

Author keywords

1,4 Dihydropyridine; Alzheimer's disease; BACE 1 inhibitors; Hydroxyethylamine

Indexed keywords

1,4 DIHYDROPYRIDINE DERIVATIVE; ALKALINE PHOSPHATASE; AMIDE; BENZYL 1 (3 ACETOXYPROPYL) 5 [4 (CYCLOPROPYLAMINO) 3 HYDROXY 1 PHENYLBUTAN 2 YLCARBAMOYL] 2,4,6 TRIMETHYL 1,4 DIHYDROPYRIDINE 3 CARBOXYLATE; BENZYL 5 [4 (CYCLOPROPYLAMINO) 3 HYDROXY 1 PHENYL BUTAN 2 YLCARBAMOYL] 1 (2 ETHOXY 2 OXOETHYL) 2,4,6 TRIMETHYL 1,4 DIHYDROPYRIDINE 3 CARBOXYLATE; BENZYL 5 [4 (CYCLOPROPYLAMINO) 3 HYDROXY 1 PHENYL BUTAN 2 YLCARBAMOYL] 1 (2 ISOPROPOXY 2 OXOETHYL) 2,4,6 TRIMETHYL 1,4 DIHYDROPYRIDINE 3 CARBOXYLATE; BENZYL 5 [4 (CYCLOPROPYLAMINO) 3 HYDROXY 1 PHENYL BUTAN 2 YLCARBAMOYL] 1 (2 METHOXY 2 OXOETHYL) 2,4,6 TRIMETHYL 1,4 DIHYDROPYRIDINE 3 CARBOXYLATE; BENZYL 5 [4 (CYCLOPROPYLAMINO) 3 HYDROXY 1 PHENYL BUTAN 2 YLCARBAMOYL] 1 [2 (DIMETHYLAMINO) 2 OXOETHYL] 2,4,6 TRIMETHYL 1,4 DIHYDROPYRIDINE 3 CARBOXYLATE; BENZYL 5 [4 (CYCLOPROPYLAMINO) 3 HYDROXY 1 PHENYL BUTAN 2 YLCARBAMOYL] 2,4,6 TRIMETHYL 1 (METHYLSULFONYL) 1,4 DIHYDROPYRIDINE 3 CARBOXYLATE; BENZYL 5 [4 (CYCLOPROPYLAMINO) 3 HYDROXY 1 PHENYL BUTAN 2 YLCARBAMOYL] 2,6 DIMETHYL 1 (METHYLSULFONYL) 4 PHENYL 1,4 DIHYDROPYRIDINE 3 CARBOXYLATE; BENZYL 5 [4 (CYCLOPROPYLAMINO) 3 HYDROXY 1 PHENYL BUTAN 2 YLCARBAMOYL] 2,6 DIMETHYL 1 (METHYLSULFONYL) 4 PROPYL 1,4 DIHYDROPYRIDINE 3 CARBOXYLATE; BENZYL 5 [4 (CYCLOPROPYLAMINO) 3 HYDROXY 1 PHENYL BUTAN 2 YLCARBAMOYL] 4 ETHYL 2,6 DIMETHYL 1 (METHYLSULFONYL) 1,4 DIHYDROPYRIDINE 3 CARBOXYLATE; BENZYL 5 [4 (CYCLOPROPYLAMINO) 3 HYDROXY 1 PHENYL BUTAN 2 YLCARBAMOYL] 4 ISOPROPYL 2,6 DIMETHYL 1 (METHYLSULFONYL) 1,4 DIHYDROPYRIDINE 3 CARBOXYLATE; BENZYL 5 [4 (CYCLOPROPYLAMINO) 3 HYDROXY 1 PHENYLBUTAN 2 YLCARBAMOYL] 1 (2 ISOPROPOXY 2 OXOETHYL) 2,4 DIMETHYL 1,4 DIHYDROPYRIDINE 3 CARBOXYLATE; BENZYL 5 [4 (CYCLOPROPYLAMINO) 3 HYDROXY 1 PHENYLBUTAN 2 YLCARBAMOYL] 1 [2 [ISOPROPYL(METHYL)AMINO] 2 OXOETHYL] 2,4,6 TRIMETHYL 1 (2 MORPHOLINO 2 OXOETHYL) 1,4 DIHYDROPYRIDINE 3 CARBOXYLATE; BENZYL 5 [4 (CYCLOPROPYLAMINO) 3 HYDROXY 1 PHENYLBUTAN 2 YLCARBAMOYL] 2,4,6 TRIMETHYL 1 (2 MORPHOLINO 2 OXOETHYL) 1,4 DIHYDROPYRIDINE 3 CARBOXYLATE; BETA SECRETASE; BETA SECRETASE INHIBITOR; ETHYLAMINE; HYBRID PROTEIN; HYDROXYETHYLAMINE; ISOPHTHALAMIDE; ISOPROPYL 2 [3 ACETYL 5 [3 HYDROXY 4 (3 METHOXY BENZYLAMINO) 1 PHENYLBUTAN 2 YLCARBAMOYL] 2,6 DIMETHYL 4 PROPYLPYRIDIN 1 (4H) YL]ACETATE; ISOPROPYL 2 [3 ACETYL 5 [3 HYDROXY 4 (3 METHOXY PHENYLAMINO) 1 PHENYLBUTAN 2 YLCARBAMOYL] 2,6 DIMETHYL 4 PROPYLPYRIDIN 1 (4H) YL]ACETATE; ISOPROPYL 2 [3 ACETYL 5 [4 (3 FLUOROPHENYLAMINO) 3 HYDROXY 1 PHENYLBUTAN 2 YLCARBAMOYL] 2,4,6 TRIMETHYLPYRIDIN 1 (4H) YL]ACETATE; ISOPROPYL 2 [3 ACETYL 5 [4 (3 FLUOROPHENYLAMINO) 3 HYDROXY 1 PHENYLBUTAN 2 YLCARBAMOYL] 2,6 DIMETHYL 4 PROPYLPYRIDIN 1 (4H) YL]ACETATE; ISOPROPYL 2 [3 ACETYL 5 [4 (CYCLOPROPYLAMINO) 3 HYDROXY 1 PHENYLBUTAN 2 YLCARBAMOYL] 2,4,6 TRIMETHYLPYRIDIN 1 (4H) YL]ACETATE; N3 [4 (CYCLOPROPYLAMINO) 3 HYDROXY 1 PHENYL BUTAN 2 YL] 2,4,6 TRIMETHYL 1 (METHYLSULFONYL) N5 (1 PHENYL ETHYL) 1,4 DIHYDROPYRIDINE 3,5 DICARBOXAMIDE; N3 [4 (CYCLOPROPYLAMINO) 3 HYDROXY 1 PHENYL BUTAN 2 YL] 4 ETHYL 2,6 DIMETHYL 1 (METHYLSULFONYL) N5 (1 PHENYL ETHYL) 1,4 DIHYDROPYRIDINE 3,5 DICARBOXAMIDE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ARTICLE; BRAIN; CELL ASSAY; COMPUTER AIDED DESIGN; CONTROLLED STUDY; DRUG ACTIVITY; DRUG DESIGN; DRUG SCREENING; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HUMAN CELL; IC 50; MOLECULAR DOCKING; PROTEIN CLEAVAGE;

AMYLOID PRECURSOR PROTEIN SECRETASES; ASPARTIC ACID ENDOPEPTIDASES; CELL LINE; DIHYDROPYRIDINES; DRUG DESIGN; INHIBITORY CONCENTRATION 50; MODELS, MOLECULAR; MOLECULAR CONFORMATION;

EID: 77950811650     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2010.02.046     Document Type: Article

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