2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i,e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, to a patient in need of such therapy.
揭示了能够减少中性粒细胞在炎症或免疫反应期间导致有害氧自由基形成的化合物,包括2,5-二芳基
四氢呋喃、2,5-二芳基
四氢噻吩、1,3-二芳基
环戊烷。这些化合物通过作为PAF受体拮抗剂、抑制5-脂氧合酶酶或表现出双重活性(即既作为PAF受体拮抗剂又作为5-脂氧合酶
抑制剂)来展示这种
生物活性。还揭示了一种治疗由PAF和/或
白三烯介导的疾病的方法,包括向需要此类治疗的患者投予上述化合物或其药学上可接受的盐中的一个或多个的有效量,可选地在药学上可接受的载体中。