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

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 functional...

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Published inJournal of medicinal chemistry Vol. 27; no. 2; pp. 125 - 128
Main Authors Honma, Yasushi, Hanamoto, Kyoji, Hashiyama, Tomiki, Sekine, Yasuo, Takeda, Mikio, Ono, Yasutoshi, Tsuzurahara, Kei
Format Journal Article
LanguageEnglish
Published United States American Chemical Society 01.02.1984
Subjects
Animals
Biological Assay
Chemical Phenomena
Chemistry
Hypersensitivity - drug therapy
Niacinamide - analogs & derivatives
Niacinamide - chemical synthesis
Niacinamide - pharmacology
Passive Cutaneous Anaphylaxis - drug effects
Rats
Structure-Activity Relationship
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Summary: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.
Bibliography:istex:D6ECC362717EA18B78154E5C1A17C610678030AB
ark:/67375/TPS-CBSZXZLM-V
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00368a005