1,2,4-三唑并[4,3-a]喹喔啉-1,4-二酮作为抗过敏剂。
1,2,4-Triazolo[4,3-a]quinoxaline-1,4-diones as antiallergic agents.
作者信息
Loev B, Musser J H, Brown R E, Jones H, Kahen R, Huang F C, Khandwala A, Sonnino-Goldman P, Leibowitz M J
出版信息
J Med Chem. 1985 Mar;28(3):363-6. doi: 10.1021/jm00381a016.
A series of new 1,4-dihydro-1,2,4-triazolo[4,3-]quinoxaline-1,4-diones has been prepared. These compounds were tested as inhibitors of antigen-induced release of histamine (AIR) in vitro from rat peritoneal mast cells (RMC) and as inhibitors of IgE-mediated rat passive cutaneous anaphylaxis (PCA). Most of this new class of antiallergic agents showed good activity in the RMC and PCA tests. The most potent compound, 2-acetyl-7-chloro-5-n-propyl-1,2,4-triazolo[4,3-a]quinoxaline-1,4-dione (1x), with an I50 value of 0.1 microM, is 30 times more potent than disodium cromoglycate (DSCG) in the RMC assay.
已经制备了一系列新的1,4 - 二氢 - 1,2,4 - 三唑并[4,3 - a]喹喔啉 - 1,4 - 二酮。这些化合物作为抗原诱导的大鼠腹膜肥大细胞（RMC）体外组胺释放（AIR）抑制剂以及IgE介导的大鼠被动皮肤过敏反应（PCA）抑制剂进行了测试。这类新型抗过敏剂中的大多数在RMC和PCA测试中表现出良好的活性。最有效的化合物2 - 乙酰基 - 7 - 氯 - 5 - 正丙基 - 1,2,4 - 三唑并[4,3 - a]喹喔啉 - 1,4 - 二酮（1x），I50值为0.1 microM，在RMC测定中比色甘酸二钠（DSCG）强30倍。
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