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新型大鼠被动皮肤过敏反应口服活性抑制剂：N-[2-(4-吡啶基)-4-嘧啶基]脲和二烷基[[[2-(4-吡啶基)-4-嘧啶基]氨基]亚甲基]丙二酸酯。

Novel orally active inhibitors of passive cutaneous anaphylaxis in rats: N-[2-(4-pyridinyl)-4-pyrimidinyl]ureas and dialkyl [[[2-(4-pyridinyl)-4-pyrimidinyl]amino]methylene]malonates.

作者信息

Lesher G Y, Singh B, Mielens Z E

出版信息

J Med Chem. 1982 Jul;25(7):837-42. doi: 10.1021/jm00349a014.

DOI:10.1021/jm00349a014
PMID:6180166
Abstract

4-Chloro-2-(4-pyridinyl)pyrimidines were treated with alkylamines to afford the corresponding N-substituted amino derivatives. 4-Amino-2-(4-pyridinyl)pyrimidines and their N-substituted analogues were converted to amides, carbamates, aminomethylenemalonates, and ureas. Many of these compounds were found to have potential antiallergic activity as indicated by the rat passive cutaneous anaphylaxis screen. The most compounds were found in the last two series.

摘要

将4-氯-2-(4-吡啶基)嘧啶与烷基胺反应，得到相应的N-取代氨基衍生物。4-氨基-2-(4-吡啶基)嘧啶及其N-取代类似物被转化为酰胺、氨基甲酸酯、氨基亚甲基丙二酸酯和脲。大鼠被动皮肤过敏反应筛选表明，这些化合物中的许多具有潜在的抗过敏活性。在最后两个系列中发现的化合物最多。

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