Abstract
A series of meta-substituted anilines were designed and synthesized to inhibit the interaction of LFA-1 with ICAM for the treatment of autoimmune disease. Design of these molecules was performed by utilizing a co-crystal structure for structure-based drug design. The resulting molecules were found to be potent and to possess favorable pharmaceutical properties.
MeSH terms
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Administration, Oral
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Aniline Compounds / chemical synthesis*
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Aniline Compounds / chemistry
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Aniline Compounds / pharmacology*
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Animals
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Chemistry, Pharmaceutical / methods*
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Combinatorial Chemistry Techniques
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Crystallography, X-Ray
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Drug Design*
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Inhibitory Concentration 50
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Intercellular Adhesion Molecule-1 / drug effects*
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Lymphocyte Function-Associated Antigen-1 / chemistry*
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Molecular Conformation
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Rats
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Stereoisomerism
Substances
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Aniline Compounds
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Lymphocyte Function-Associated Antigen-1
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Intercellular Adhesion Molecule-1