Synthesis and SAR study of new thiazole derivatives as vascular adhesion protein-1 (VAP-1) inhibitors for the treatment of diabetic macular edema: Part 2

Bioorganic and Medicinal Chemistry

Volumn 21, Issue 9, 2013, Pages 2478-2494

  Inoue, Takayuki ^a   Morita, Masataka ^a   Tojo, Takashi ^a   Nagashima, Akira ^a   Moritomo, Ayako ^a   Imai, Keisuke ^a   Miyake, Hiroshi ^a  

^a ASTELLAS PHARMA INC   (Japan)

Author keywords

Guanidine; Homology model; Hybrid; Inhibitor; Sequence information; Species difference; VAP 1

Indexed keywords

2 METHYL 4 [4 (METHYLSULFANYL)BENZYLIDENE] 1,3 OXAZOL 5(4H) ONE; 3 [4 (METHYLSULFANYL)PHENYL] 1H PYRAZOL 5 AMINE; 3 [4 (METHYLSULFANYL)PHENYL] 2 OXOPROPANOIC ACID; 3 [4 (METHYLSULFANYL)PHENYL] 3 OXOPROPANENITRILE; ETHYL 2 (ACETYLAMINO) 5 [3 (METHYLTHIO)BENZYL] 1,3 THIAZOLE 4 CARBOXYLATE; ETHYL 2 (ACETYLAMINO) 5 [4 (METHYLTHIO)BENZYL] 1,3 THIAZOLE 4 CARBOXYLATE; ETHYL 2 (ACETYLAMINO) 5 BENZYL 1,3 THIAZOLE 4 CARBOXYLATE; ETHYL 2 AMINO 5 [3 (METHYLTHIO)BENZYL] 1,3 THIAZOLE 4 CARBOXYLATE; ETHYL 2 AMINO 5 [4 (METHYLTHIO)BENZYL] 1,3 THIAZOLE 4 CARBOXYLATE; ETHYL 2 AMINO 5 BENZYL 1,3 THIAZOLE 4 CARBOXYLATE; ETHYL 3 BROMO 2 OXO 4 PHENYLBUTANOATE; ETHYL 3 BROMO 4 [3 (METHYLTHIO)PHENYL] 2 OXOBUTANOATE; ETHYL 3 BROMO 4 [4 (METHYLTHIO)PHENYL] 2 OXOBUTANOATE; ETHYL 4 [3 (METHYLTHIO)PHENYL] 2 OXOBUTANOATE; ETHYL 4 [4 (METHYLTHIO)PHENYL] 2 OXOBUTANOATE; METHYL 2 (ACETYLAMINO) 5 [4 (METHYLTHIO)PHENYL] 1,3 THIAZOLE 4 CARBOXYLATE; METHYL 2 AMINO 5 [4 (METHYLTHIO)PHENYL] 1,3 THIAZOLE 4 CARBOXYLATE; METHYL 3 [3 (METHYLSULFANYL)PHENYL]ACRYLATE; METHYL 3 [3 (METHYLTHIO)PHENYL]PROPANOATE; METHYL 3 [4 (METHYLSULFANYL)PHENYL] 2 OXOPROPANOATE; METHYL 3 [4 (METHYLTHIO)PHENYL]PROPANOATE; METHYL 3 BROMO 3 [4 (METHYLSULFANYL)PHENYL] 2 OXOPROPANOATE; N [1 [2 (4 CARBAMIMIDAMIDOPHENYL)ETHYL] 5 [4 (METHYLSULFONYL)PHENYL] 1H PYRAZOL 3 YL]ACETAMIDE HYDROCHLORIDE; N [3 [4 (METHYLSULFANYL)PHENYL] 1H PYRAZOL 5 YL]ACETAMIDE; N [4 FORMYL 5 [4 (METHYLSULFANYL)PHENYL] 1,3 THIAZOL 2 YL]ACETAMIDE; N [4 FORMYL 5 [4 (METHYLTHIO)BENZYL] 1,3 THIAZOL 2 YL]ACETAMIDE; N METHOXY N METHYL 3 (METHYLSULFANYL)BENZAMIDE; THIAZOLE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG; VASCULAR ADHESION PROTEIN 1;

ACETYLATION; ARTICLE; BROMINATION; CYCLIZATION; DIABETIC MACULAR EDEMA; DRUG DESIGN; DRUG EFFICACY; DRUG SELECTIVITY; DRUG SYNTHESIS; ENZYME ACTIVITY; ESTERIFICATION; HIGH THROUGHPUT SCREENING; HUMAN; HYDROGENATION; IC 50; MOLECULAR DOCKING; NONHUMAN; SEQUENCE HOMOLOGY; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

AMINE OXIDASE (COPPER-CONTAINING); ANIMALS; CELL ADHESION MOLECULES; DIABETIC RETINOPATHY; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; MACULAR EDEMA; MODELS, MOLECULAR; MOLECULAR STRUCTURE; RATS; RATS, WISTAR; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZOLES;

RATTUS;

EID: 84876120372     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2013.02.048     Document Type: Article

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