Ltd(4) Receptor-Binding Activity Of Novel Pyridine Chromanols - Qualitative Correlation With Pk(A)

A series of pyridine chromanols were synthesized and evaluated as LTD(4)-antagonists (LTD(4)-A). The quinoline sidechain of this class of such agents, as exemplified by REV-5901, has until now been deemed as essential for potent activity. However, by manipulating substituents on a pyridine ring, quinoline-like potency can be achieved. The results indicate that this is a function of pKa.