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LTD4 Receptor binding activity of novel pyridine chromanols: qualitative correlation with pKa

1995; Elsevier BV; Volume: 5; Issue: 13 Linguagem: Inglês

10.1016/0960-894x(95)00226-j

1464-3405

Hiroko Masamune, James F. Eggler, Anthony Marfat, Lawrence S. Melvin, Frank W. Rusek, Jeanene E. Tickner, John B. Cheng, John T. Shirley,

DNA and Nucleic Acid Chemistry

A series of pyridine chromanols were synthesized and evaluated as LTD4-antagonists (LTD4-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.