Harper R W, Herron D K, Bollinger N G, Sawyer J S, Baldwin R F, Roman C R, Rinkema L E, Fleisch J H
Eli Lilly and Company, Indianapolis, Indiana 46285.
J Med Chem. 1992 Apr 3;35(7):1191-200. doi: 10.1021/jm00085a004.
A hypothetical model for receptor binding of leukotriene D4 (LTD4) was deduced from conformational analysis of LTD4 and from the structure-activity relationships (SAR) of known LTD4 receptor antagonists. A new structural series of LTD4 receptor antagonists exemplified by 5-[4-(4-phenylbutoxy)phenyl]-2-[4-(tetrazol-5-yl)butyl]-2H-t etrazole was designed in which a phenyltetrazole moiety was incorporated as a receptor binding equivalent of the triene unit of LTD4. A number of these phenyltetrazoles were prepared and found to possess LTD4 receptor antagonist activity. The structure-activity relationship (SAR) of this series is described.
