（E）-3-[6-[[(2,6-二氯苯基)硫代]甲基]-3-(2-苯乙氧基)-2-吡啶基]-2-丙烯酸：一种具有口服抗炎活性的高亲和力白三烯B4受体拮抗剂。
(E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist with oral antiinflammatory activity.
作者信息
Daines R A, Chambers P A, Foley J J, Griswold D E, Kingsbury W D, Martin L D, Schmidt D B, Sham K K, Sarau H M
机构信息
Department of Medicinal Chemistry, SmithKline Beecham Pharmaceuticals, King of Prussia, Pennsylvania 19406-0939, USA.
出版信息
J Med Chem. 1996 Sep 13;39(19):3837-41. doi: 10.1021/jm960248s.
An extensive structure-activity study based around the high-affinity leukotriene B4 (LTB4) 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 LTB4 receptor (Ki = 0.78 nM), blocks LTB4-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.
围绕高亲和力白三烯B4（LTB4）受体拮抗剂SB 201146（1）开展的广泛构效关系研究，促成了（E）-3-[6-[[(2,6-二氯苯基)-硫代]甲基]-3-(2-苯乙氧基)-2-吡啶基]-2-丙烯酸（3）的发现。该化合物对人中性粒细胞LTB4受体具有高亲和力（Ki = 0.78 nM），以6.6±1.5 nM的IC50阻断LTB4诱导的Ca2+动员，并在皮肤炎症小鼠模型中表现出强效的口服和局部抗炎活性。
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