Design and synthesis of dipeptide nitriles as reversible and potent cathepsin S inhibitors

Journal of Medicinal Chemistry

Volumn 45, Issue 25, 2002, Pages 5471-5482

  Ward, Yancey D ^a   Thomson, David S ^a   Frye, Leah L ^a,b   Cywin, Charles L ^a   Morwick, Tina ^a   Emmanuel, Michel J ^a   Zindell, Renée ^a   McNeil, Daniel ^a   Bekkali, Younes ^a   Giradot, Marc ^a,c   Hrapchak, Matt ^a   DeTuri, Molly ^a,d   Crane, Kathy ^a   White, Della ^a   Pav, Susan ^a   Wang, Yong ^a,e   Hao, Ming Hong ^a   Grygon, Christine A ^a   Labadia, Mark E ^a   Freeman, Dorothy M ^a   Davidson, Walter ^a   Hopkins, Jerry L ^a   Brown, Maryanne L ^a   Spero, Denice M ^a   more..

^a BOEHRINGER INGELHEIM PHARMACEUTICALS INC   (United States)

^b SCHRÖDINGER INC   (United States)

^c ASTRAZENECA   (United Kingdom)

^d BRISTOL MYERS SQUIBB COMPANY   (United States)

^e ELI LILLY AND COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CATHEPSIN S; ENZYME INHIBITOR; MORPHOLINE 4 CARBOXYLIC ACID[(CYANO 2 METHYLPROPYLCARBAMOYL) 3 METHYLBUTYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[(CYANO 2 PHENYLETHYLCARBAMOYL) 3 METHYLBUTYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[(CYANO 2,2 DIMETHYLPROPYLCARBAMOYL) 3 METHYLBUTYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[(CYANO 3 PHENYLPROPYLCARBAMOYL) 1,3 DIMETHYLBUTYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[(CYANO 3 PHENYLPROPYLCARBAMOYL) 2 CYCLOHEXYLETHYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[(CYANO 3 PHENYLPROPYLCARBAMOYL) 2 METHYLPROPYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[(CYANO 3 PHENYLPROPYLCARBAMOYL) 2 PHENYLETHYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[(CYANO 3 PHENYLPROPYLCARBAMOYL) 3 METHYLBUTYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[(CYANO 3 PHENYLPROPYLCARBAMOYL) 3,3 DIMETHYLBUTYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[(CYANO 3 PHENYLPROPYLCARBAMOYL)3 METHYLBUTYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[(CYANO 3 PHENYLPROPYLCARBAMOYL)CYCLOHEXYLMETHYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[(CYANO 3 PHENYLPROPYLCARBAMOYL)ETHYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[(CYANO 3 PHENYLPROPYLCARBAMOYL)PENTYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[(CYANOBUTYLCARBAMOYL) 3 METHYLBUTYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[(CYANOETHYLCARBAMOYL) 3 METHYLBUTYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[(CYANOPENTYLCARBAMOYL) 3 METHYLBUTYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[3 METHYL (1 PROP 2 YNYLCARBAMOYL)BUTYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[3 METHYL (3 PHENYL)PROPYLCARBAMOYL)BUTYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[3 METHYL(METHYL 3 PHENYLPROPYLCARBAMOYL)BUTYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[[(1 CYANO 1 METHYL)ETHYLCARBAMOYL] 3 METHYLBUTYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[[(CYANOPHENYLMETHYL)CARBAMOYL] 3 METHYLBUTYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[[2 (2 CHLOROBENZYLOXY)CYANOETHYLCARBAMOYL] 3 METHYLBUTYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[[2 (3 CHLOROBENZYLOXY)CYANOETHYLCARBAMOYL] 3 METHYLBUTYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[[2 (4 CHLOROBENZYLOXY)CYANOETHYLCARBAMOYL] 3 METHYLBUTYL]AMIDE; MORPHOLINE 4 CARBOXYLIC ACID[[CYANO 2 (3,4 DICHLOROPHENYL)ETHYLCARBAMOYL] 3 METHYLBUTYL]AMIDE; NITRILE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANTIGEN PRESENTATION; ARTICLE; CONTROLLED STUDY; CRYSTAL STRUCTURE; CRYSTALLIZATION; DIASTEREOISOMER; DRUG DESIGN; DRUG POTENCY; DRUG SYNTHESIS; ENZYME ACTIVITY; ENZYME INHIBITION; HUMAN; HUMAN CELL; IC 50; IMMUNE RESPONSE; STRUCTURE ACTIVITY RELATION; T LYMPHOCYTE ACTIVATION;

B-LYMPHOCYTES; BINDING, COMPETITIVE; CATHEPSINS; CELL LINE; CRYSTALLOGRAPHY, X-RAY; DIPEPTIDES; ENZYME INHIBITORS; HUMANS; KINETICS; MODELS, MOLECULAR; NITRILES; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0037028023     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm020209i     Document Type: Article

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