Hughes P, DeVirgilio J, Humber L G, Chau T, Weichman B, Neuman G
Wyeth-Ayerst Research, Princeton, New Jersey 08543-8000.
J Med Chem. 1989 Sep;32(9):2134-7. doi: 10.1021/jm00129a018.
The synthesis of 4,6-diethyl-1,3,4,5-tetrahydropyrano[4,3-b]indole-4-acetic acid, an isomer of the antiinflammatory agent etodolac, is described. The compound was found to have an ED50 of 3 mg/kg po in the rat curative adjuvant arthritis assay, and an IC50 of 50 nM for inhibiting prostaglandin production in cultured chondrocytes.
描述了抗炎药依托度酸的异构体4,6 - 二乙基 - 1,3,4,5 - 四氢吡喃并[4,3 - b]吲哚 - 4 - 乙酸的合成。在大鼠佐剂性关节炎治疗试验中，该化合物经口服给药的半数有效剂量（ED50）为3mg/kg，在培养的软骨细胞中抑制前列腺素产生的半数抑制浓度（IC50）为50nM。
