Design, synthesis, and evaluation of Leu*Ala hydroxyethylene-based non-peptide β-secretase (BACE) inhibitors

Bioorganic and Medicinal Chemistry

Volumn 14, Issue 13, 2006, Pages 4535-4551

  Xiao, Kun ^a   Li, Xin ^a   Li, Jingya ^b   Ma, Lanping ^a   Hu, Bin ^a   Yu, Haiping ^b   Fu, Yan ^a   Wang, Rui ^a   Ma, Zeqiang ^b   Qiu, Beiying ^b   Li, Jia ^b   Hu, Dingyu ^a   Wang, Xin ^a   Shen, Jingkang ^a  

^a SHANGHAI INSTITUTE OF MATERIA MEDICA   (China)

^b National Center for Drug Screening   (China)

Author keywords

BACE; Combinatorial synthesis; Hydrogen bond; Non peptide inhibitor

Indexed keywords

4 ((4 HYDROXY 5 (N 3, N 3 DIPROPYLISOPHTHALAMIDO) 2,7 DIMETHYLOCTANOYLAMINO)METHYL)CYCLOHEXANECARBOXYLIC ACID; 4 ((4 HYDROXY 5 (N 3, N 3 DIPROPYLISOPHTHALAMIDO) 2,7 DIMETHYLOCTANOYLAMINO)METHYL)CYCLOHEXANECARBOXYLIC ACID METHYL ESTER; AMINE; BETA SECRETASE INHIBITOR; ETHYLENE DERIVATIVE; ISOBUTYL AMINE; LEUCYLALANINE HYDROXYETHYLENE; METHYL(METHYLSULFONYL)AMINE; N 1 (7 (1 HYDROXY 3 METHYLBUTAN 2 YLCARBAMOYL) 5 HYDROXY 2 METHYL 4 YL) N 3, N 3 DIPROPYLISOPHTHALAMIDE; N 1 (7 (1 HYDROXY 3 PHENYLPROPAN 2 YLCARBAMOYL) 5 HYDROXY 2 METHYL 4 YL) N 3, N 3 DIPROPYLISOPHTHALAMIDE; N 1 (7 (2 (TRIFLUOROMETHYL)BENZYLCARBAMOYL) 5 HYDROXY 2 METHYL 4 YL) N 3, N 3 DIPROPYLISOPHTHALAMIDE; N 1 (7 (2,3 DIHYDROXYPROPYLCARBAMOYL) 5 HYDROXY 2 METHYL 4 YL) N 3, N 3 DIPROPYLISOPHTHALAMIDE; N 1 (7 (3 (TRIFLUOROMETHYL)BENZYLCARBAMOYL) 5 HYDROXY 2 METHYL 4 YL) N 3, N 3 DIPROPYLISOPHTHALAMIDE; N 1 (7 (BENZYLCARBAMOYL) 5 HYDROXY 2 METHYL 4 YL) N 3, N 3 DIPROPYLISOPHTHALAMIDE; N 1 (7 (ISOBUTYLCARBAMOYL) 5 HYDROXY 2 METHYL 4 YL) N 3, N 3 DIPROPYLISOPHTHALAMIDE; N 1 (7 (ISOBUTYLCARBAMOYL) 5 HYDROXY 2 METHYLOCTAN 4 YL) 5 (METHYL(METHYLSULFONYL)AMINE) N 3, N 3 DIPROPYLBENZENE 1,3 DIAMIDE; N 1 (7 (ISOBUTYLCARBAMOYL) 5 HYDROXY 2 METHYLOCTAN 4 YL) 5 NITRO N 3, N 3 DIPROPYLBENZENE 1,3 DIAMIDE; N 1 (7 (ISOBUTYLCARBAMOYL) 5 HYDROXY 2 METHYLOCTAN 4 YL) N 3 ((4 PHENYLPIPERAZIN) 1 YL)ISOPHTHALAMIDE; N 1 (7 (ISOBUTYLCARBAMOYL) 5 HYDROXY 2 METHYLOCTAN 4 YL) N 3 ((NAPHTHALEN 1 YL)METHYL)ISOPHTHALAMIDE; N 1 (7 (ISOBUTYLCARBAMOYL) 5 HYDROXY 2 METHYLOCTAN 4 YL) N 3 (1 HYDROXY 3 METHYLBUTAN 2 YL)ISOPHTHALAMIDE; N 1 (7 (ISOBUTYLCARBAMOYL) 5 HYDROXY 2 METHYLOCTAN 4 YL) N 3 (1 HYDROXY 3 PHENYLPROPAN 2 YL)ISOPHTHALAMIDE; N 1 (7 (ISOBUTYLCARBAMOYL) 5 HYDROXY 2 METHYLOCTAN 4 YL) N 3 (1,2,2,3 DDIHYDRO 2 HYDROXY 1H INDEN 1 YL)ISOPHTHALAMIDE; N 1 (7 (ISOBUTYLCARBAMOYL) 5 HYDROXY 2 METHYLOCTAN 4 YL) N 3 (2,3 DIHYDRO 1H INDEN 1 YL)ISOPHTHALAMIDE; N 1 (7 (ISOBUTYLCARBAMOYL) 5 HYDROXY 2 METHYLOCTAN 4 YL) N 3 (2,3 DIHYDRO 1H INDEN 2 YL)ISOPHTHALAMIDE; N 1 (7 (ISOBUTYLCARBAMOYL) 5 HYDROXY 2 METHYLOCTAN 4 YL) N 3 (2,3 DIHYDRO 2 HYDROXY 1H INDEN 1 YL)ISOPHTHALAMIDE; N 1 (7 (ISOBUTYLCARBAMOYL) 5 HYDROXY 2 METHYLOCTAN 4 YL) N 3 (2,3 DIHYDROXYPROPYL)ISOPHTHALAMIDE; N 1 (7 (ISOBUTYLCARBAMOYL) 5 HYDROXY 2 METHYLOCTAN 4 YL) N 3 BENZHYDRYLISOPHTHALAMIDE; N 1 (7 (ISOBUTYLCARBAMOYL) 5 HYDROXY 2 METHYLOCTAN 4 YL) N 3 BENZYLISOPHTHALAMIDE; NITRO(METHYLSULFONYL)AMINE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

AMINO TERMINAL SEQUENCE; ARTICLE; CARBOXY TERMINAL SEQUENCE; CONTROLLED STUDY; DRUG BINDING SITE; DRUG DESIGN; DRUG IDENTIFICATION; DRUG INHIBITION; DRUG POTENCY; DRUG SCREENING; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HUMAN CELL; HYDROGEN BOND; IC 50; MOLECULAR MODEL; MOLECULAR WEIGHT; STRUCTURE ACTIVITY RELATION;

AMYLOID PRECURSOR PROTEIN SECRETASES; ASPARTIC ENDOPEPTIDASES; BENZAMIDES; CARBAMATES; DIPEPTIDES; DRUG DESIGN; ENDOPEPTIDASES; ETHYLENES; HUMANS; MOLECULAR STRUCTURE; NITROBENZENES; OLIGOPEPTIDES; PEPTIDES; PROTEASE INHIBITORS;

EID: 33646733845     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2006.02.024     Document Type: Article

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