4H-Imidazo[2,1-c][1,4]benzoxazine-2-carboxylic acid (3) was found to possess potent activity in the IgE-induced rat passive cutaneous anaphylaxis model which may be predictive of clinical antiallergic activity. Compared to disodium cromoglycate (DSCG, 1), 3 was less active following iv administration but unlike DSCG showed very significant oral activity. To explore the structural requirements for this activity, a range of tricyclic compounds was prepared and their activities were measured. Individual 2-carboxylic acids derived from imidazo[1,2-a]quinolines, imidazo[1,2-a]quinoxalines, imidazo[1,2-a]quinoxalinones, pyrrolo[1,2-a]quinoxalinones, pyrrolo[2,3-a]quinoxalinones, and imidazo[2,1-b]benzothiazoles showed iv activities up to 10(3) times as potent as DSCG and many of them showed significant oral activity. From these, imidazo[1,2-a]quinoxaline-2-carboxylic acid 114 has been chosen for further development.

中文翻译：

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咪唑并[2,1-c] [1,4]苯并恶嗪，咪唑并[1,2-a]喹啉，咪唑并[1,2-a]喹喔啉，咪唑并[1,2]的羧酸的合成及口服抗过敏活性-a]喹喔啉，吡咯并[1,2-a]喹喔啉，吡咯并[2,3-a]喹喔啉和咪唑并[2,1-b]苯并噻唑。

在IgE诱导的大鼠被动皮肤过敏反应模型中，发现4H-咪唑并[2,1-c] [1,4]苯并恶嗪-2-羧酸（3）具有有效的活性，这可能预示了临床抗过敏活性。与色甘酸二钠（DSCG，1）相比，静脉注射后3的活性较低，但与DSCG不同，口服活性非常高。为了探索该活性的结构要求，制备了一系列三环化合物并测量了它们的活性。分别由咪唑并[1,2-a]喹啉，咪唑并[1,2-a]喹喔啉，咪唑并[1,2-a]喹喔啉，吡咯并[1,2-a]喹喔啉，吡咯并[2]衍生的2-羧酸，3-a]喹喔啉酮和咪唑并[2,1-b]苯并噻唑类药物的iv活性高达DSCG的10（3）倍，其中许多具有明显的口服活性。从这些，咪唑[1，