Novel molecules that antagonize leukotriene B4 binding to neutrophils.
A series of LTB4 analogues have been synthesized that replace carbons 7-9 of the cis-trans-trans triene unit of LTB4 with a stable ring structure. Meta-substituted pyridine analogues are more potent inhibitors than benzene or furan analogues. C-1 alcohols are often more potent inhibitors than free carboxylic acids, and 5,6-cis double bond compounds are more potent than 5,6-trans compounds. Compounds such as these may prove to be useful in the treatment of inflammatory diseases.
Lin
A H
AH
Cell Biology and Metabolic Diseases Research, Upjohn Company, Kalamazoo, Michigan 49001.
Morris
J
J
Wishka
D G
DG
Gorman
R R
RR
D007975:Leukotriene B4 / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors / Q000378:metabolism; D009504:Neutrophils / Q000187:drug effects* / Q000378:metabolism; D011485:Protein Binding; D011971:Receptors, Immunologic / Q000187:drug effects* / Q000378:metabolism; D018102:Receptors, Leukotriene B4; D013329:Structure-Activity Relationship
D011971:Receptors, Immunologic; D018102:Receptors, Leukotriene B4; D007975:Leukotriene B4