Development of a Series of Phenyltetrazole Leukotriene D4(LTD4) Receptor Antagonist

Article abstract of 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-tetrazole 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.