Background: 3-Amino-4-(2,4,5-trifluorophenyl) butyric acid has potential pharmacological effects in promoting insulin secretion. Menthol promotes drug transdermal absorption and hypoglycemic effects. Objective: The objective of the study was to combine the 3-amino-4-(2,4,5- trifluorophenyl) butyric acid and menthol to develop a new candidate drug molecule that can be used as a hypoglycemic drug in type II diabetes. Methods: In this study, the molecular structure of 3-amino-4-(2,4,5-trifluorophenyl) butyric acid in sitagliptin was modified by replacing pyrazine imidazole with menthol. The structure of the target compound was characterized by nuclear magnetic resonance (NMR). The anti-diabetic activity of BHF in N000180 BKS.Cg-Dock7m+/ +Leprdb/Nju mice with spontaneous diabetes was preliminarily studied. Results: A potential multi-target drug molecule, 3-amino-4-(2,4,5-trifluorophenyl) butyrate (BHF), was synthesized by combining 3-amino-4-(2,4,5-trifluorophenyl) butyric acid and menthol. BHF is suitable for hyperglycemic mice and has a significant hypoglycemic effect; the low dose of 10 mg/kg-1 started to be effective, and the high dose of 40 mg/kg-1 was more effective than the positive drug metformin. Conclusion: In this study, BHF has been synthesized and presented significant antidiabetic activities.

中文翻译：

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3-氨基-4-（2,4,5-三氟苯基）丁酸薄荷酯的制备及其降血糖活性的研究


背景： 3-氨基-4-（2,4,5-三氟苯基）丁酸在促进胰岛素分泌方面具有潜在的药理作用。薄荷醇促进药物透皮吸收和降血糖作用。目的： 本研究旨在将 3-氨基-4-（2,4,5-三氟苯基）丁酸与薄荷醇结合，开发一种新的候选药物分子，可用作 II 型糖尿病的降糖药。方法： 本研究通过用薄荷醇取代吡嗪咪唑来修饰西格列汀中 3-氨基-4-（2,4,5-三氟苯基）丁酸的分子结构。通过核磁共振 （NMR） 表征目标化合物的结构。BHF 在 N000180 BKS 中的抗糖尿病活性。初步研究了患有自发性糖尿病的 Cg-Dock7m+/ +Leprdb/Nju 小鼠。结果： 通过将 3-氨基-4-（2,4,5-三氟苯基）丁酸和薄荷醇组合合成了一种潜在的多靶点药物分子 3-氨基-4-（2,4,5-三氟苯基）丁酸酯 （BHF）。BHF 适用于高血糖小鼠，具有显着的降血糖作用;10 mg/kg-1 的低剂量开始有效，40 mg/kg-1 的高剂量比阳性药物二甲双胍更有效。结论： 在本研究中，BHF 已被合成并表现出显着的抗糖尿病活性。