Tiwari Ashok K, Kumbhare Ravindra M, Agawane Sachin B, Ali Amtul Z, Kumar K Vijay
Pharmacology Division, Taranaka, Indian Institute of Chemical Technology, Hyderabad 500607, India.
Bioorg Med Chem Lett. 2008 Jul 15;18(14):4130-2. doi: 10.1016/j.bmcl.2008.05.088. Epub 2008 May 27.
A series of beta-acetamido carbonyl compounds (S(1)-S(7)) were prepared using Dakin-West reaction from different substituted aldehyde and acetophenone in the presence of lanthanum triflate as a solid catalyst. All the compounds were tested for their alpha-glucosidase inhibitory potential against rat intestinal alpha-glucosidase. The most potent rat intestinal alpha-glucosidase inhibitors S(5) and S(7) were tested for their antihyperglycemic activity following carbohydrate tolerance test. Both the compounds displayed antihyperglycemic activity equivalent to the standard drug acarbose.
使用达金-韦斯特反应,以三氟甲磺酸镧作为固体催化剂,由不同取代的醛和苯乙酮制备了一系列β-乙酰氨基羰基化合物(S(1)-S(7))。测试了所有化合物对大鼠肠道α-葡萄糖苷酶的α-葡萄糖苷酶抑制潜力。对最有效的大鼠肠道α-葡萄糖苷酶抑制剂S(5)和S(7)进行了碳水化合物耐量试验后的降血糖活性测试。这两种化合物均表现出与标准药物阿卡波糖相当的降血糖活性。