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目的研究2-羟基-5-丁酰胺基苯甲酸合成方法及其抗溃疡性结肠炎的作用。方法以5-氨基水杨酸为原料,与丁酰氯反应,而后水解,合成2-羟基-5-丁酰胺基苯甲酸。采用大鼠乙酸性结肠炎模型研究2-羟基-5-丁酰胺基苯甲酸的抗溃疡性结肠炎的作用。结果经IR和1HNMR分析证明合成产物为2-羟基-5-丁酰胺基苯甲酸。结肠炎大鼠给予2-羟基-5-丁酰胺基苯甲酸,可减轻乙酸性结肠炎大鼠的结肠粘膜损伤指数和粪便隐血程度,降低MPO水平,并可改善结肠粘膜病理损伤。结论2-羟基-5-丁酰胺基苯甲酸合成工艺简单,条件温和;而且2-羟基-5-丁酰胺基苯甲酸具有抗溃疡性结肠炎的作用。
Objective To study the synthesis of 2-hydroxy-5-butyrylaminobenzoic acid and its anti-ulcerative colitis. Methods 5-Aminosalicylic acid was used as a starting material to react with butyryl chloride and then hydrolyzed to synthesize 2-hydroxy-5-butyrylaminobenzoic acid. Effect of 2-hydroxy-5-butyrylaminobenzoic acid on ulcerative colitis in rat model of acetic acid-induced colitis. Results IR and 1H NMR analysis showed that the product was 2-hydroxy-5-butyrylaminobenzoic acid. Colitis rats given 2-hydroxy-5-butyrylaminobenzoic acid, can reduce the acetic acid-induced colitis mucosal injury index and fecal occult blood levels, reduce the level of MPO, and can improve the pathological damage of colonic mucosa. Conclusion 2-hydroxy-5-butyrylaminobenzoic acid synthesis process is simple, mild conditions; and 2-hydroxy-5-butylamido-benzoic acid has anti-ulcerative colitis role.