A series of N-aryl cinnamides has been prepared and assayed for antagonism of the leukotriene B4receptor. Several compounds in this series were found to be highly potent antagonists of the human neutrophil receptor, based on a whole cell binding assay, as well as a neutrophil aggregation assay. This series is unique among LTB4antagonists, due to its high degree of rigidity.
Greenspan, P. D., Main, A. J., Bhagwat, S. S., Barsky, L. I., Doti, R. A., Engle, A. R., … Uziel-Fusi, S. (1997). N-Aryl cinnamides: A novel class of rigid and highly potent leukotriene B4receptor antagonists. Bioorganic and Medicinal Chemistry Letters, 7(7), 949–954. https://doi.org/10.1016/S0960-894X(97)00134-0