Journal of Medicinal Chemistry 1984-02-01

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

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

Index: J. Med. Chem. 27(2) , 125-28, (1984)

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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.