The discovery of CP-96,021 and CP-96,486, balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonists.
作者: Melvin, L. ; Copper, K. ; Masamune, H. ; Chambers, R. ; Watson, J. ; Cheng, J. ; Delehunt, J. ; Egger, J. ; Marfat, A. ; Damon, D.
The combination of key structural pharmacophores found in known leukotriene D4 (LTD4) receptor antagonists with those of potent platelet activating factor (PAF) receptor antagonist UK-74,505 has led to the synthesis of hybrid compounds CP-96,021 and CP-96,486.These compounds represent the first known balanced, combined and orally active LTD4/PAF receptor antagonists.The use of these compounds to treat asthma is discussed.