新型小分子白细胞介素-8（IL-8）受体拮抗剂3,5-二芳基异恶唑和3,5-二芳基-1,2,4-恶二唑的合成及其构效关系
Synthesis and structure-activity relationships of 3,5-diarylisoxazoles and 3,5-diaryl-1,2,4-oxadiazoles, novel classes of small molecule interleukin-8 (IL-8) receptor antagonists.
作者信息
Weidner-Wells Michele A, Henninger Todd C, Fraga-Spano Stephanie A, Boggs Christine M, Matheis Michele, Ritchie David M, Argentieri Dennis C, Wachter Michael P, Hlasta Dennis J
机构信息
Johnson and Johnson Pharmaceutical Research and Development, LLC 1000 Route 202, Raritan, NJ 08869, USA.
出版信息
Bioorg Med Chem Lett. 2004 Aug 16;14(16):4307-11. doi: 10.1016/j.bmcl.2004.05.080.
A novel series of 3,5-diarylisoxazole and 3,5-diaryl-1,2,4-oxadiazole IL-8 inhibitors has been identified. These compounds exhibit activity in an IL-8 binding assay as well as in a functional assay of IL-8 induced elastase release from neutrophils. In addition, one of the compounds exhibits oral activity in a rat adjuvant arthritis model.
已鉴定出一系列新型的3,5 - 二芳基异恶唑和3,5 - 二芳基 - 1,2,4 - 恶二唑白细胞介素 - 8抑制剂。这些化合物在白细胞介素 - 8结合试验以及白细胞介素 - 8诱导中性粒细胞释放弹性蛋白酶的功能试验中均表现出活性。此外，其中一种化合物在大鼠佐剂性关节炎模型中表现出口服活性。
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