Carboxy-substituted cinnamides: a novel series of potent, orally active LTB4 receptor antagonists
…, R Pelletier, S Uziel-Fusi, RH Jackson…
文献索引：Greenspan, Paul D.; Fujimoto, Roger A.; Marshall, Paul J.; Raychaudhuri, Anil; Lipson, Kenneth E.; Zhou, Huanghai; Doti, Robert A.; Coppa, David E.; Zhu, Lijuan; Pelletier, Roberta; Uziel-Fusi, Susan; Jackson, Robert H.; Chin, Michael H.; Kotyuk, Bernard L.; Fitt, John J. Journal of Medicinal Chemistry, 1999 , vol. 42, # 1 p. 164 - 172
A series of carboxy-substituted cinnamides were investigated as antagonists of the human cell surface leukotriene B4 (LTB4) receptor. Binding was determined through measurement of [3H] LTB4 displacement from human neutrophils. Receptor antagonism was confirmed through a functional assay, which measures inhibition of Ca2+ release in human neutrophils. Potent antagonists were discovered through optimization of a random ...
