A series of substituted 11-oxo-11H-pyrido[2,1-b]quinazoline-8-carboxylic acids were prepared and evaluated as antiallergy agents. Several analogues were orally active. 2-Methyl-11-oxo-11H-pyrido[2,1-b]quinoazoline-8-carboxylic acid (6) was superior to cromolyn sodium and doxantrazole orally and intravenously in the rat PCA test and a rat allergic bronchospasm model.

A new series of 11-oxo-11H-pyrido[2,1-b]quinazolinecarboxylic acids and related analogues has been synthesized and evaluated as potential antiallergy agents. In the rat PCA test, 11-oxo-11H-pyrido[2,1--b]quinazoline-8-carboxylic acid is orally active and more potent than cromolyn sodium or doxantrazole intravenously.

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kindly provided the antitumor screening results, and the Walter Reed Institute of Medical Research provided the results of the antimalarial tests.

A new selective P-adrenergic stimulant 3-[~-(tert-butylamino)methyl]-5-hydroxy-m-xylene-ol,ol'-diol was prepared from dimethyl 5-hydroxyisophthalate in several steps. This agent possesses the structural features of salbutamol and terbutaline responsible for their selective &-stimulant action. It was found that this analog was selective as a / 3 stimulant in the tracheas of dogs and guinea pigs but was less potent than either salbutamol or terbutaline.