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由于色甘酸钠的剂量太大(20mg/kg),不能通过剂量吸入器给药,因而不适用于儿童和易受刺激引起支气管痉挛的病人。要解决这一问题必须把药效提高100～300倍,使剂量降至0.2～0.07mg/kg。作者合成了三组吡唑并[5,1-b]喹唑啉-9-酮的衍生物,并研究了它们对小鼠皮肤被动变态反应(PCA)的抑制作用。结果发现了一些活性比色甘酸钠强得多的化合物。尤其是化合物36(熔点271～272°)。PCA实验结果表明,静脉给药0.1mg/kg时的抑制率为100%,0.01mg/kg时抑制率为74%,活性约为色甘酸钠的250倍,有可能作为气雾剂用于治疗哮喘。其合成方法的概括流程为,将2-氨基-3-甲氧基苯甲酰肼与草酰醋酸
Because cromolyn is administered in too large a dose (20 mg / kg), it can not be administered by a metered dose inhaler and is therefore not suitable for use in children and in patients susceptible to bronchospasm. To solve this problem must improve the efficacy of 100 to 300 times, so that the dose dropped to 0.2 ~ 0.07mg / kg. The authors synthesized three derivatives of pyrazolo [5,1-b] quinazolin-9-one and investigated their inhibitory effects on mouse skin passive anaphylaxis (PCA). As a result, some compounds were found to be much more active than cromolyn. In particular, compound 36 (melting point 271-272 °). The results of PCA showed that the inhibition rate was 100% when administered intravenously at 0.1mg / kg, the inhibition rate was 74% at 0.01mg / kg, and the activity was about 250 times that of cromolyn sodium, which may be used as an aerosol for treatment asthma. The general procedure for its synthesis is as follows: A mixture of 2-amino-3-methoxybenzohydrazide and oxaloacetate