Synthesis and biological evaluation of benzoic acid derivatives as potent, orally active VLA-4 antagonists

Bioorganic and Medicinal Chemistry

Volumn 15, Issue 4, 2007, Pages 1679-1693

  Chiba, Jun ^a   Iimura, Shin ^a   Yoneda, Yoshiyuki ^a   Watanabe, Toshiyuki ^a   Muro, Fumito ^a   Tsubokawa, Masao ^a   Iigou, Yutaka ^a   Satoh, Atsushi ^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 [3 BROMO 4 [N' (2 BROMOPHENYL)UREIDO]PHENYLACETYL] FLUOROPYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [3 BROMO 4 [N' (2 CHLOROPHENYL)UREIDO]PHENYLACETYL] FLUOROPYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [3 BROMO 4 [N' (2 METHYLPHENYL)UREIDO]PHENYLACETYL] FLUOROPYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [3 CHLORO 4 [N' (2 CHLOROPHENYL)UREIDO]PHENYLACETYL] FLUOROPYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [3 CHLORO 4 [N' (2 METHYLPHENYL)UREIDO]PHENYLACETYL] FLUOROPYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [3 ETHYL 4 [N' (2 METHYLPHENYL)UREIDO] 3 METHYLPHENYLACETYL] FLUOROPYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [3 ISOPROPYL 4 [N' (2 METHYLPHENYL)UREIDO] 3 METHYLPHENYLACETYL] FLUOROPYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [4 [N' (2 BROMOPHENYL)UREIDO] 3 CHLOROPHENYLACETYL] FLUOROPYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [4 [N' (2 BROMOPHENYL)UREIDO] 3 METHOXYPHENYLACETYL] FLUOROPYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [4 [N' (2 BROMOPHENYL)UREIDO] 3 METHYLPHENYLACETYL] FLUOROPYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [4 [N' (2 CHLOROPHENYL)UREIDO] 3 METHOXYPHENYLACETYL] FLUOROPYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [4 [N' (2 CHLOROPHENYL)UREIDO] 3 METHYLPHENYLACETYL] FLUOROPYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [1 [4 [N' (2 METHYLPHENYL)UREIDO] 3 TRIFLUOROMETHYLPHENYLACETYL] FLUOROPYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [FLUORO 1 [3 METHOXY 4 [N' (2 TRIFLUOROMETHYLPHENYL)UREIDO] 3 METHOXYPHENYLACETYL]FLUOROPYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [FLUORO 1 [3 METHYL 4 [N' (2 METHYLPHENYL)UREIDO] 3 METHOXYPHENYLACETYL]FLUOROPYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [FLUORO 1 [4 [N' (2 ISOPROPYLPHENYL)UREIDO] 3 METHOXYPHENYLACETYL] FLUOROPYRROLIDINYLMETHOXY]BENZOIC ACID; 4 [FLUORO 1 [4 [N' (2 METHOXYPHENYL)UREIDO] 3 METHOXYPHENYLACETYL] FLUOROPYRROLIDINYLMETHOXY]BENZOIC ACID; BENZENE; BENZOIC ACID DERIVATIVE; BROMINE; CHLORINE; RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG; UREA DERIVATIVE; VERY LATE ACTIVATION ANTIGEN 4 ANTAGONIST;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DOG; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; FEMALE; IC 50; MALE; MOUSE; NONHUMAN; RAT;

ADMINISTRATION, ORAL; ANIMALS; BENZOIC ACIDS; DISEASE MODELS, ANIMAL; DOGS; INFLAMMATION; INHIBITORY CONCENTRATION 50; INTEGRIN ALPHA4BETA1; MICE; PHARMACOKINETICS; PLEURISY; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

CANIS FAMILIARIS; MUS; RATTUS;

EID: 33847770256     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2006.12.006     Document Type: Article

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