Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors

European Journal of Medicinal Chemistry

Volumn 46, Issue 6, 2011, Pages 2058-2065

  Ettari, Roberta ^a   Zappalà, Maria ^a   Micale, Nicola ^a   Grazioso, Giovanni ^b   Giofrè, Salvatore ^a   Schirmeister, Tanja ^c   Grasso, Silvana ^a  

^a UNIVERSITY OF MESSINA   (Italy)

^b UNIVERSITY OF MILAN   (Italy)

^c UNIVERSITY OF WÜRZBURG   (Germany)

Author keywords

Cysteine proteases; Docking studies; Falcipain 2 inhibitors; Peptidomimetics

Indexed keywords

2 (OXO 5 PHENYL 3 PIPERIDIN 1 YL METHYL 2,3 DIHYDRO BENZO[E][1,4] DIAZEPIN 1 YL) ACETIC ACID ETHYL ESTER; 2 (OXO 5 PHENYL 3 PIPERIDIN 1 YLMETHYL 2,3 DIHYDRO BENZO[E][1,4] DIAZEPIN 1 YL)ACETIC ACID; 2 [3 (ISOBUTYLAMINO METHYL) 2 OXO 5 PHENYL 2,3 DIHYDRO BENZO[E][1,4]DIAZEPIN 1 YL] N (4 OXO PENT 2 ENYL)ACETAMIDE; 3 (HYDROXYMETHYL 2 OXO 5 PHENYL 2,3 DIHYDRO BENZO[E][1,4]DIAZEPIN 1 YL) ACETIC ACID ETHYL ESTER; 3 (MORPHOLIN 4 YL METHYL 2 OXO 5 PHENYL 2,3 DIHYDRO BENZO[E][1,4] DIAZEPIN 1 YL) ACETIC ACID ETHYL ESTER; 3 (MORPHOLIN 4 YLMETHYL 2 OXO 5 PHENYL 2,3 DIHYDRO BENZO[E][1,4]DIAZEPIN 1 YL)ACETIC ACID; 3 (TERT BUTYL DIMETHYL SILANYLOXYMETHYL) 5 METHYL 1,3 DIHYDRO BENZO[E][1,4]DIAZEPIN 2 ONE; 3 [(ISOBUTYLAMINO METHYL) 2 OXO 5 PHENYL 2,3 DIHYDRO BENZO[E][1,4] DIAZEPIN 1 YL] ACETIC ACID ETHYL ESTER; 3 [(ISOBUTYLAMINO METHYL) 2 OXO 5 PHENYL 2,3 DIHYDRO BENZO[E][1,4] DIAZEPIN 1 YL]ACETIC ACID; 3 HYDROXYMETHYL 5 METHYL 1,3 DIHYDROBENZO[E][1,4]DIAZEPIN 2 ONE; 4 (2 BENZOYL METHYLCARBAMOYL) 2,2 DIMETHYL OXAZOLIDINE 3 CARBOXYLIC ACID TERT BUTYL ESTER; CATHEPSIN B; CYSTEINE PROTEINASE; FALCIPAIN 2; KETONE; N (4 OXO PENT 2 ENYL) 2 (2 OXO 5 PHENYL 3 MORPHOLIN 1 YL METHYL 2,3 DIHYDRO BENZO[E][1,4]DIAZEPIN 1 YL)ACETAMIDE; N (4 OXO PENT 2 ENYL) 2 (2 OXO 5 PHENYL 3 PIPERIDIN 1 YL METHYL 2,3 DIHYDRO BENZO[E][1,4] DIAZEPIN 1 YL)ACETAMIDE; N ALLYL 2 (2 OXO 5 PHENYL 3 PIPERIDIN 1 YL METHYL 2,3 DIHYDRO BENZO[E][1,4]DIAZEPIN 1 YL)ACETAMIDE; N ALLYL 2 (3 MORPHOLIN 4 YLMETHYL 2 OXO 5 PHENYL 2,3 DIHYDRO BENZO[E][1,4]DIAZEPIN 1 YL)ACETAMIDE; N ALLYL 2 [3 (ISOBUTYLAMINO METHYL) 2 OXO 5 PHENYL 2,3 DIHYDRO BENZO[E][1,4]DIAZEPIN 1 YL]ACETAMIDE; PEPTIDOMIMETIC AGENT; UNCLASSIFIED DRUG;

ARTICLE; CARBON NUCLEAR MAGNETIC RESONANCE; DRUG SYNTHESIS; ENZYME ACTIVITY; PROTON NUCLEAR MAGNETIC RESONANCE; STRUCTURE ACTIVITY RELATION;

BENZODIAZEPINONES; CYSTEINE ENDOPEPTIDASES; CYSTEINE PROTEINASE INHIBITORS; DRUG DESIGN; ENZYME ACTIVATION; HUMANS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PEPTIDOMIMETICS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 79955623446     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2011.02.058     Document Type: Article

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