INHIBITORY EFFECT AND STRUCTURE-ACTIVITY RELATIONSHIP OF EBSELEN DERIVATIVES ON LEUKOTRIENE B₄ BIOSYNTHESIS

AIM: A series of ebselen derivatives were synthesized for studying their effects on LTB4 biosynthesis. Preliminary analysis of structure-activity relationship(SAR) of these compounds were conducted. METHODS: High performance liquid chromatography(HPLC) was used to determine LTB₄. RESULTS: Sulfonamide analogues of ebselen and N-aryl substituted derivatives of ebselen showed significant inhibitory effects on LTB4 biosynthesis with IC₅₀ of 10-5 mol.L^-1 to 10^-6 mol.L^-1.CONCLUSION: According to SAR, the presence of an acidic hydrogen atom on the sulfonamido group seemed to be a critical factor for the activity. In the absence of the hydrogen or loss of the ability to form intermolecular hydrogen bonding compounds would abolish the activity.