Identification of 4-[1-[3-chloro-4-[N'-(5-fluoro-2-methylphenyl)ureido]phenylacetyl]-(4S)-fluoro-(2S)-pyrrolidinylmethoxy]benzoic acid as a potent, orally active VLA-4 antagonist

Bioorganic and Medicinal Chemistry

Volumn 16, Issue 23, 2008, Pages 9991-10000

  Muro, Fumihito ^a   Iimura, Shin ^a   Yoneda, Yoshiyuki ^a   Chiba, Jun ^a   Watanabe, Toshiyuki ^a   Setoguchi, Masaki ^a   Iigou, Yutaka ^a   Takayama, Gensuke ^a   Yokoyama, Mika ^a   Takashi, Tohru ^a   Nakayama, Atsushi ^a   Machinaga, Nobuo ^a  

^a DAIICHI SANKYO CO   (Japan)

Author keywords

Integrin; Oral availability; VLA 4

Indexed keywords

4 [1 [2,5 DICHLORO 4 [N' (2 METHYLPHENYL)UREIDO]PHENYLACETYL]FLUORO PYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [3 CHLORO 4 [N' (2 CHLOROPHENYL)UREIDO] 6 FLUOROPHENYLACETYL]FLUORO PYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [3 CHLORO 4 [N' (3 FLUORO 2 METHYLPHENYL)UREIDO]PHENYLACETYL]FLUORO PYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [3 CHLORO 4 [N' (4 FLUORO 2 METHYLPHENYL)UREIDO]PHENYLACETYL]FLUORO PYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [3 CHLORO 4 [N' (5 FLUORO 2 METHYLPHENYL)UREIDO]PHENYLACETYL]FLUORO PYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [3 CHLORO 6 FLUORO 4 [N' (2 METHYLPHENYL)UREIDO]PHENYLACETYL]FLUORO PYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [4 [N' (2 BROMOPHENYL)UREIDO] 2,5 DICHLOROPHENYLACETYL]FLUORO PYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [4 [N' (2 BROMOPHENYL)UREIDO] 3 CHLORO 6 FLUOROPHENYLACETYL]FLUORO PYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [4 [N' (2 BROMOPHENYL)UREIDO] 5 CHLORO 2 METHYLPHENYLACETYL]FLUORO PYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [4 [N' (2 CHLOROPHENYL)UREIDO] 2,5 DICHLOROPHENYLACETYLFLUORO PYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [5 CHLORO 4 [N' (2 CHLOROPHENYL)UREIDO] 3 METHYLPHENYLACETYL]FLUORO PYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [5 CHLORO 4 [N' (2 METHYLPHENYL)UREIDO] 2 METHYLPHENYLACETYL]FLUORO PYRROLIDINYLMETHOXY]BENZOIC ACID; BENZOIC ACID DERIVATIVE; UNCLASSIFIED DRUG; VASCULAR CELL ADHESION MOLECULE 1; VERY LATE ACTIVATION ANTIGEN 4;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIINFLAMMATORY ACTIVITY; AREA UNDER THE CURVE; ARTICLE; ASTHMA; BLOOD SAMPLING; CELL INFILTRATION; CELL MEMBRANE PERMEABILITY; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG IDENTIFICATION; DRUG SYNTHESIS; EOSINOPHIL; FEMALE; HUMAN; HUMAN CELL; HYDROLYSIS; LUNG LAVAGE; MALE; MOUSE; NONHUMAN; PHYSICAL CHEMISTRY; PROTEIN BINDING; RAT; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; ANTI-INFLAMMATORY AGENTS; ASTHMA; BENZOIC ACIDS; CELLS, CULTURED; DISEASE MODELS, ANIMAL; DOGS; FEMALE; INHIBITORY CONCENTRATION 50; INTEGRIN ALPHA4BETA1; MICE; MICE, INBRED BALB C; PERMEABILITY; PYRROLES; RATS;

MURINAE;

EID: 55749092767     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2008.10.020     Document Type: Article

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