Development of potent dipeptide-type SARS-CoV 3CL protease inhibitors with novel P3 scaffolds: Design, synthesis, biological evaluation, and docking studies

European Journal of Medicinal Chemistry

Volumn 68, Issue , 2013, Pages 372-384

  Thanigaimalai, Pillaiyar ^a   Konno, Sho ^a   Yamamoto, Takehito ^a   Koiwai, Yuji ^a   Taguchi, Akihiro ^a   Takayama, Kentaro ^a   Yakushiji, Fumika ^a   Akaji, Kenichi ^b   Chen, Shen En ^c   Naser Tavakolian, Aurash ^c   Schön, Arne ^c   Freire, Ernesto ^c   Hayashi, Yoshio ^a  

^a TOKYO UNIVERSITY OF PHARMACY AND LIFE SCIENCES   (Japan)

^b KYOTO PHARMACEUTICAL UNIVERSITY   (Japan)

^c JOHNS HOPKINS UNIVERSITY   (United States)

Author keywords

Cysteine protease inhibitors; Dipeptide; Peptidomimetics; SARS

Indexed keywords

CARBONYL DERIVATIVE; N ( 1 (( 1 (BENZO[D]THIAZOL 2 YL) 1 OXO 3 ( 2 OXOPYRROLIDIN 3 YL)PROPA 2 YL)AMINO) 4 METHYL 1 OXOPENTAN 2 YL) 4 HYDROXY 1H INDOLE 2 CARBOXAMIDE; N ( 1 (( 1 (BENZO[D]THIAZOL 2 YL) 1 OXO 3 ( 2 OXOPYRROLIDIN 3 YL)PROPAN 2 YL)AMINO) 4 METHYL 1 OXOPENTAN 2 YL) 4 ISOPROPOXY 1H INDOLE 2 CARBOXAMIDE; N ( 1 (( 1 (BENZO[D]THIAZOL 2 YL) 1 OXO 3 ( 2OXOPYRROLIDIN 3 YL)PROPAN 2 YL)AMINO) 4 METHYL 1 OXOPENTAN 2 YL) 4 METHOXY 1H INDOLE 2 CARBOXAMIDE; N (1 ) ((1 (BENZO[D]THIAZOL 2 YL) 1 OXO 3 2 OXOPYRROLIDIN 3 YL)PROPAN 2 YL) 1H INDOLE 2 CARBOXAMIDE; N (1) ((1 (BENZO[D]THIAZOL 2 YL) 1 OXO 3 ( 2 OXOPYRROLIDIN 3 YL)PROPAN 2 YL)AMINO) 4 METHYL 1 OXOPENTA 2 YL) 6 METHOXY 1H INDOLE CARBOXAMIDE; N (1) ((1 (BENZO[D]THIAZOL 2 YL) 1 OXO 3 ( 2 OXOPYRROLIDIN 3 YL)PROPAN 2 YL)AMINO) 4 METHYL 1 OXOPENTAN 2 YL) 5 HYDROXY 1H INDOLE 2 CARBOXAMIDE; N (1) ((1 (BENZO[D]THIAZOL 2 YL) 1 OXO 3 (2 OXOPYRROLIDIN 3 YL)PROPAN 2 YL) 4 METHYL 1 OXOPENTAN 2 YL) 5 CHLORO 1H INDOLE 2 CARBOXAMIDE; N (1) ((1 (BENZO[D]THIAZOL 2 YL) 1 OXO 3 (2 OXOPYRROLIDIN 3 YL)PROPAN 2 YL)AMINO) 4 METHYL 1 OXOPENTAN 2 YL) 5 METHOXY 1H INDOLE 2 CARBOXAMIDE; UNCLASSIFIED DRUG;

ARTICLE; DRUG DESIGN; DRUG SYNTHESIS; IC 50; ISOTHERMAL TITRATION CALORIMETRY; MOLECULAR DOCKING; STRUCTURE ACTIVITY RELATION;

CYSTEINE PROTEASE INHIBITORS; DIPEPTIDE; PEPTIDOMIMETICS; SARS; SARS-COV 3CL(PRO);

CYSTEINE ENDOPEPTIDASES; DRUG DESIGN; ENZYME ACTIVATION; INHIBITORY CONCENTRATION 50; MOLECULAR DOCKING SIMULATION; PROTEASE INHIBITORS; SARS VIRUS; STRUCTURE-ACTIVITY RELATIONSHIP; VIRAL PROTEINS;

EID: 84882798645     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2013.07.037     Document Type: Article

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