抗过敏药。3. N-(1H-四唑-5-基)-2-吡啶甲酰胺。

Antiallergic agents. 3. N-(1H-tetrazol-5-yl)-2-pyridinecarboxamides.

作者信息

Honma Y, Hanamoto K, Hashiyama T, Sekine Y, Takeda M, Ono Y, Tsuzurahara K

出版信息

J Med Chem. 1984 Feb;27(2):125-8. doi: 10.1021/jm00368a005.

Abstract

A series of N-tetrazolylpyridinecarboxamides was prepared and evaluated for antiallergic activity by the passive cutaneous anaphylaxis (PCA) assay. From the structure-activity relationships (SAR) of this class of compounds, it was revealed that the N-tetrazolylcarbamoyl group as an acidic functionality is required to be at the 2-position of the pyridine nucleus and that the phenyl group as a subtituent is not necessarily required for activity. 6-Methyl-N-(1H-tetrazol-5-yl)-2-pyridinecarboxamide (36) showed good oral activity and low toxicity.

摘要

制备了一系列N-四唑基吡啶甲酰胺，并通过被动皮肤过敏反应（PCA）试验评估其抗过敏活性。从这类化合物的构效关系（SAR）可知，作为酸性官能团的N-四唑基甲酰基需位于吡啶核的2-位，且作为取代基的苯基对于活性并非必需。6-甲基-N-(1H-四唑-5-基)-2-吡啶甲酰胺（36）显示出良好的口服活性和低毒性。