喹啉-2-羧酸四环衍生物的抗过敏活性。1.
Antiallergic activity of tetracyclic derivatives of quinoline-2-carboxylic acids. 1.
作者信息
Erickson E H, Lappi L R, Rice T K, Swingle K F, Van Winkle M
出版信息
J Med Chem. 1978 Sep;21(9):984-8. doi: 10.1021/jm00207a026.
Substitution of 1,4-dihydro-4-oxoquinoline-2-carboxylic acid by acetyl, benzoyl, and phenylsulfonyl substituents was found to enhance activity in the rat passive cutaneous anaphylaxis assay. A further increase in activity, to equipotency with DSCG, was achieved by incorporation of the 8-benzoyl moiety into a tetracyclic structure to give 1,4-dihydro-4,11(1H,11H)-dioxoindeno[1,2-h]quinoline-2-carboxylic acid (20). In contrast, the reverse isomer 19 was found to have little activity.
研究发现，用乙酰基、苯甲酰基和苯磺酰基取代1,4 - 二氢 - 4 - 氧代喹啉 - 2 - 羧酸可增强其在大鼠被动皮肤过敏反应试验中的活性。通过将8 - 苯甲酰基部分引入四环结构中得到1,4 - 二氢 - 4,11(1H,11H) - 二氧代茚并[1,2 - h]喹啉 - 2 - 羧酸（20），活性进一步提高，达到了与色甘酸钠等效的效力。相比之下，发现其反式异构体19几乎没有活性。
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