抗过敏药。2. N-（1H-四唑-5-基）-6-苯基-2-吡啶甲酰胺。
Antiallergic agents. 2. N-(1H-tetrazol-5-yl)-6-phenyl-2-pyridinecarboxamides.
作者信息
Honma Y, Oda K, Hashiyama T, Hanamoto K, Nakai H, Inoue H, Ishida A, Takeda M, Ono Y, Tsuzurahara K
出版信息
J Med Chem. 1983 Oct;26(10):1499-504. doi: 10.1021/jm00364a026.
A new series of N-(1H-tetrazol-5-yl)-6-phenyl-2-pyridinecarboxamides was prepared to determine the effects of substituents on the benzene and pyridine rings on antiallergic activity in the rat passive cutaneous anaphylaxis (PCA) assay after oral administration. One member of this series, N-(1H-tetrazol-5-yl)-4-methyl-6-[4-(methylamino)-phenyl]-2- pyridinecarboxamide (231), has an ED50 value of 0.8 mg/kg po and is 85 times more potent than disodium cromoglycate (DSCG) on intravenous administration. Further evaluation of 231 as a clinically useful antiallergic agent is in progress.
制备了一系列新的N-(1H-四唑-5-基)-6-苯基-2-吡啶甲酰胺，以确定苯环和吡啶环上的取代基对大鼠被动皮肤过敏反应（PCA）试验中口服给药后抗过敏活性的影响。该系列中的一个成员，N-(1H-四唑-5-基)-4-甲基-6-[4-(甲氨基)-苯基]-2-吡啶甲酰胺（231），口服给药的半数有效剂量（ED50）值为0.8mg/kg，静脉给药时比色甘酸钠二钠（DSCG）强85倍。目前正在对231作为一种临床有用的抗过敏药物进行进一步评估。
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