An extensive structure-activity study based around the high-affinity leukotriene B-4 (LTB(4)) receptor antagonist SB 201146 (1) led to the identification of (E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2-pyridinyl]-2-propenoic acid (3). This compound displays high affinity for the human neutrophil LTB(4) receptor (K-i = 0.78 nM), blocks LTB(4)-induced Ca2+ mobilization with an IC50 of 6.6 +/- 1.5 nM, and demonstrates potent oral and topical antiinflammatory activity in a murine model of dermal inflammation.
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页码:3837 / 3841
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[1]
BOYUM A, 1968, SCAND J CLIN LAB INV, VS 21, P77