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Discovery and SAR of diarylsulfide cyclopropylamide LFA-1/ICAM-1 interaction antagonists.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2001 Apr 23; Vol. 11 (8), pp. 973-6. - Publication Year :
- 2001
-
Abstract
- Diarylsulfide cyclopropylamides were synthesized and evaluated as LFA-1/ICAM-1 interaction antagonists. A substituent pattern was identified which maximized potency and minimized protein binding as exemplified by antagonist 30 (IC50 = 5 nM).
- Subjects :
- Administration, Oral
Amides chemical synthesis
Animals
Area Under Curve
Biological Availability
Cell Communication physiology
Endothelium cytology
Endothelium metabolism
Inhibitory Concentration 50
Intercellular Adhesion Molecule-1 metabolism
Leukocytes metabolism
Lymphocyte Function-Associated Antigen-1 metabolism
Protein Binding physiology
Rats
Structure-Activity Relationship
Amides pharmacology
Cell Communication drug effects
Cyclopropanes chemical synthesis
Cyclopropanes pharmacology
Intercellular Adhesion Molecule-1 drug effects
Lymphocyte Function-Associated Antigen-1 drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 11
- Issue :
- 8
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 11327603
- Full Text :
- https://doi.org/10.1016/s0960-894x(01)00105-6