10-氧代-10H-吡啶并[1,2-a]噻吩并[3,2-d]嘧啶和10-氧代-10H-吡啶并[1,2-a]噻吩并[3,4-d]嘧啶的合成及抗过敏活性
Synthesis and antiallergy activity of 10-oxo-10H-pyrido[1,2-a]thieno[3,2-d]pyrimidines and 10-oxo-10H-pyrido[1,2-a]thieno[3,4-d]pyrimidines.
作者信息
Connor D T, Sorenson R J, Cetenko W A, Kerbleski J J, Tinney F J
出版信息
J Med Chem. 1984 Apr;27(4):528-30. doi: 10.1021/jm00370a016.
Synthesis and antiallergy activity of 10-oxo-10H-pyrido[1,2-a]thieno[3,2-d]pyrimidines (2 and 3) and 10-oxo-10H-pyrido[1,2-a]thieno[3,4-d]pyrimidines (4 and 5) are described. The activity, shown by these compounds in the rat passive cutaneous anaphylaxis (PCA) test, is compared to the PCA data previously reported for a series of 4-oxo-4H-pyrido[1,2-a]thieno[2,3-d]pyrimidines. 10-Oxo-N-1H-tetrazol-5-yl-10H-pyrido[1,2-a]thieno[3,4-d]pyri midine (2b), 10-oxo-7-(1H-tetrazol-5-yl)-10H-pyrido[1,2-a]thieno[3,4-d]py rimidine (4e), and 3,10-dihydro-10-oxo-7-(1H-tetrazol-5-yl)-1H-pyrido[1,2-a]thieno[3, 4-d] pyrimidine (7e) gave a 100% inhibition in the rat PCA test at a dose of 5 mg/kg. The activity displayed by these compounds is comparable to that of the most active compounds in the 4-oxo-4H-pyrido[1,2-a]thieno[2,3-d]pyrimidine series.
描述了10-氧代-10H-吡啶并[1,2-a]噻吩并[3,2-d]嘧啶（2和3）以及10-氧代-10H-吡啶并[1,2-a]噻吩并[3,4-d]嘧啶（4和5）的合成及抗过敏活性。将这些化合物在大鼠被动皮肤过敏反应（PCA）试验中显示的活性与先前报道的一系列4-氧代-4H-吡啶并[1,2-a]噻吩并[2,3-d]嘧啶的PCA数据进行了比较。10-氧代-N-1H-四唑-5-基-10H-吡啶并[1,2-a]噻吩并[3,4-d]嘧啶（2b）、10-氧代-7-(1H-四唑-5-基)-10H-吡啶并[1,2-a]噻吩并[3,4-d]嘧啶（4e）以及3,10-二氢-10-氧代-7-(1H-四唑-5-基)-1H-吡啶并[1,2-a]噻吩并[3,4-d]嘧啶（7e）在大鼠PCA试验中以5mg/kg的剂量产生了100%的抑制作用。这些化合物显示的活性与4-氧代-4H-吡啶并[1,2-a]噻吩并[2,3-d]嘧啶系列中活性最高的化合物相当。
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