Massil S E, Shi G Y, Klotz I M
J Pharm Sci. 1984 Dec;73(12):1851-3. doi: 10.1002/jps.2600731255.
Carboxylate substituents added to the salicylate ring increase the effectiveness of a variety of aspirins and diaspirins in acylating hemoglobin. Even more effective are a series of monoesters of dicarboxylate derivatives. Bis(5-carbomethoxysalicyl)fumarate and -succinate at 5 mM concentrations modify approximately 100% of the hemoglobin in solution and should alter the aggregation behavior of sickle hemoglobin.
添加到水杨酸环上的羧酸盐取代基可提高多种阿司匹林和双阿司匹林对血红蛋白的酰化效果。一系列二羧酸衍生物的单酯效果更佳。浓度为5 mM时,双(5 - 甲氧羰基水杨酸)富马酸酯和双(5 - 甲氧羰基水杨酸)琥珀酸酯可使溶液中约100%的血红蛋白发生改性,应该会改变镰状血红蛋白的聚集行为。