抗炎性2-苄基-4-磺酰基-4H-异喹啉-1,3-二酮：新型COX-2抑制剂
Antiinflammatory 2-benzyl-4-sulfonyl-4H-isoquinoline-1,3-diones: novel inhibitors of COX-2.
作者信息
Lazer E S, Sorcek R, Cywin C L, Thome D, Possanza G J, Graham A G, Churchill L
机构信息
Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, CT 06611, USA.
出版信息
Bioorg Med Chem Lett. 1998 May 19;8(10):1181-6. doi: 10.1016/s0960-894x(98)00184-x.
PMID:9871731
Abstract
A series of 2-benzyl-4-sulfonyl-4H-isoquinoline-1,3-diones was prepared. Members of this series are potent and selective inhibitors of cyclooxygenase-2 (COX-2) in both microsomal and cellular assays. Two representatives demonstrated activity in the carrageenan-induced paw edema model in rats upon oral administration.
摘要
制备了一系列2-苄基-4-磺酰基-4H-异喹啉-1,3-二酮。在微粒体和细胞试验中，该系列成员都是环氧合酶-2（COX-2）的强效和选择性抑制剂。两种代表性化合物经口服给药后，在角叉菜胶诱导的大鼠爪水肿模型中显示出活性。
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