Synthesis and Antiallergy Activity of [1,3,4]Thiadiazolo[3,2-α]-1,2,3-triazolo[4,5-d]pyrimidin-9(3H)-one Derivatives. II. 6-Alkyl- and 6-Cycloalkylalkyl Derivatives

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A suries of 6-alkyl- or 6-(cycloalkylalkyl)-[1,3,4]thiadiazolo[3,2-α]-1,2,3-triazolo[4,5-d]pyrimidin-9(3H)-ones 1b-o was synthesized from the corresponding 1,3,4-thiadiazol-5-animes 3b-o and the antiallergic activities of the products were evaluated. Among the compounds 6-(2-cyclohexylethyl)-[1,3,4]thiadiazolo[3,2-α]-1,2,3-triazolo[4,5-d]pyrimidin-9(3H)-one 1h, whose X-ray crystallographic stereostructure is shown, was found to be a promising new antiallergic agent, which has low toxicity and dual activity as a leukotriene D_4 receptor antagonist and as an orally active mast cell stabilizer.
公益社団法人日本薬学会の論文
1992-09-25