a-286982 and Pneumonia

a-286982 has been researched along with Pneumonia* in 1 studies

Other Studies

1 other study(ies) available for a-286982 and Pneumonia

ArticleYear
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, 2001, Dec-06, Volume: 44, Issue:25

    We have shown that p-arylthio cinnamides can inhibit the interaction of LFA-1 and ICAM-1, which is involved in cell adhesion and the inflammatory process. We now show that 2,3-disubstitution on the aryl portion of the cinnamide results in enhanced activity over mono substitution on the ring. The best 2,3-substituents were chlorine and trifluoromethyl groups. Compounds 39 and 40 which contain two CF3 groups have IC(50) values of 0.5 and 0.1 nM, respectively, in inhibiting JY8 cells expressing LFA-1 on their surface, from adhering to ICAM-1. The structure-activity relationship (SAR) was examined using an NMR based model of the LFA-1 I domain/compound 31 complex. One of our compounds (38) was able to reduce cell migration in two different in vivo experiments.

    Topics: 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

2001