Yevich J P, Temple D L, Covington R R, Owens D A, Seidehamel R J, Dungan K W
J Med Chem. 1982 Jul;25(7):864-8. doi: 10.1021/jm00349a020.
A short series of the title compounds was prepared and evaluated for both antiallergic and bronchodilator activity. Members of the series exhibit good oral activity in the rat PCA test, the most potent being the parent compound, 3-(1H-tetrazol-5-yl)-4H-pyrimido[2,1-b]benzothiazol-4-one, and its 8-chloro derivative. The latter two compounds are considerably more potent than either disodium chromoglycate or theophylline as antiallergic agents and also show significant bronchodilator activity.
制备了一小系列标题化合物，并对其抗过敏和支气管扩张活性进行了评估。该系列成员在大鼠PCA试验中表现出良好的口服活性，其中最有效的是母体化合物3-(1H-四唑-5-基)-4H-嘧啶并[2,1-b]苯并噻唑-4-酮及其8-氯衍生物。后两种化合物作为抗过敏剂比色甘酸二钠或茶碱的效力要强得多，并且还表现出显著的支气管扩张活性。
