Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intercellular adhesion molecule-1 interaction. 4. Structure - Activity relationship of substituents on the benzene ring of the cinnamide

Journal of Medicinal Chemistry

Volumn 44, Issue 25, 2001, Pages 4393-4403

  Winn, M ^a   Kester, J ^a   Von Geldern, T W ^a   Leitza, S ^a   Devries, P ^a   Dickinson, R ^a   Mussatto, D ^a   Okasinski, G F ^a   Reilly, E B ^a   Liu, G ^a   Huth, J R ^a   Jae, H S ^a   Freeman, J ^a   Pei, Z ^a   Xin, Z ^a   Lynch, J ^a  

^a ABBOTT LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

(1,4 BENZODIOXAN 6 YL)[2,3 BIS(TRIFLUOROMETHYL) 4 [(4 CARBOXYPIPERIDIN 1 YL)ETHENYL]PHENYL]SULFIDE; (2 METHOXYPHENYL)[2,3 BIS(TRIFLUOROMETHYL) 4 [[(4 CARBOXYPIPERIDIN 1 YL)CARBONYL]ETHENYL]PHENYL]SULFIDE; BENZENE; CINNAMIC ACID DERIVATIVE; INTERCELLULAR ADHESION MOLECULE 1; LYMPHOCYTE FUNCTION ASSOCIATED ANTIGEN 1; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CELL ADHESION; CONTROLLED STUDY; DRUG STRUCTURE; DRUG SYNTHESIS; IC 50; INFLAMMATION; MODEL; NONHUMAN; NUCLEAR MAGNETIC RESONANCE; RAT; REACTION ANALYSIS; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

AMIDES; ANIMALS; CELL LINE; CHEMOTAXIS, LEUKOCYTE; CINNAMATES; ENTEROTOXINS; EOSINOPHILS; INDOLES; INTERCELLULAR ADHESION MOLECULE-1; LYMPHOCYTE FUNCTION-ASSOCIATED ANTIGEN-1; MAGNETIC RESONANCE SPECTROSCOPY; MICE; MODELS, MOLECULAR; NEUTROPHILS; OVALBUMIN; PNEUMONIA; RATS; STAPHYLOCOCCUS AUREUS; STRUCTURE-ACTIVITY RELATIONSHIP; SULFIDES;

EID: 0035818921     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm0103108     Document Type: Article

References (16)

1. Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intracellular adhesion molecule-1 interaction 1. Identification of an additional binding pocket based on an anilino diaryl sulfide lead
2. Novel p-arylthio cinnamides as antagonists of LFA-1/ICAM-1 interaction. 2 Determination of the mechanism of inhibition and structure-based SAR approach for improved pharmaceutical properties
3. Discovery of potent antagonists of leukocyte function associated antigen-1/intracellular adhesion molecule-1 interaction. 3. SAR of the amide portion (C-ring) of the molecules
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