Design and synthesis of a series of meta aniline-based LFA-1 ICAM inhibitors.

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.

• Authors: Kevin M Guckian, Edward Yin-Shiang Lin, Laura Silvian, Jessica E Friedman, Donovan Chin, Daniel M Scott
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 18 Issue 19 Pg. 5249-51 (Oct 01 2008) ISSN: 1464-3405 [Electronic] England
• PMID: 18778938 (Publication Type: Journal Article)

Chemical References

• Aniline Compounds
• Lymphocyte Function-Associated Antigen-1
• Intercellular Adhesion Molecule-1

Topics

• Administration, Oral
• Aniline Compounds (chemical synthesis, chemistry, pharmacology)
• Animals
• Chemistry, Pharmaceutical (methods)
• Combinatorial Chemistry Techniques
• Crystallography, X-Ray
• Drug Design
• Inhibitory Concentration 50
• Intercellular Adhesion Molecule-1 (drug effects)
• Lymphocyte Function-Associated Antigen-1 (chemistry)
• Molecular Conformation
• Rats
• Stereoisomerism