Inhibition of α-glucosidase is an effective strategy for controlling the post-prandial hyperglycemia in diabetic patients. For the identification of new inhibitors of this enzyme, a series of new (R)-1-(2-(4-bromo-2-methoxyphenoxy) propyl)-4-(4-(trifluoromethyl) phenyl)-1H-1,2,3-triazole derivatives were synthesized (8a–d and 10a–e). The structures were confirmed by NMR, mass spectrometry and, in case of compound 8a, by single crystal X-ray crystallography. The α-glucosidase inhibitory activities were investigated in vitro. Most derivatives exhibited significant inhibitory activity against α-glucosidase enzyme. Their structure-activity relationship and molecular docking studies were performed to elucidate the active pharmacophore against this enzyme. Compound 10b was the most active analogue with IC₅₀ value of 14.2 µM, while compound 6 was found to be the least active having 218.1 µM. A preliminary structure-activity relationship suggested that the presence of 1H-1,2,3-triazole ring in 1H-1,2,3-triazole derivatives is responsible for this activity and can be used as anti-diabetic drugs. The molecular docking studies of all active compounds were performed, in order to understand the mode of binding interaction and the energy of this class of compounds.

抑制α-葡萄糖苷酶是控制糖尿病患者餐后高血糖的有效策略。为了鉴定该酶的新抑制剂，一系列新的（R）-1-（2-（4-溴-2-甲氧基苯氧基）丙基）-4-（4-（三氟甲基）苯基）-1 H -1合成了2,2,3-三唑衍生物（8a–d和10a–e）。通过NMR，质谱以及在化合物8a的情况下通过单晶X射线晶体学确认结构。的α葡萄糖苷酶抑制活性进行了研究体外。大多数衍生物对α表现出显着的抑制活性-葡糖苷酶。他们进行了结构-活性关系和分子对接研究，以阐明针对该酶的活性药效团。化合物10b是活性最高的类似物，IC ₅₀值为14.2 µM，而化合物6是活性最低的类似物，为218.1 µM。初步的结构活性关系表明，在1 H -1,2,3-三唑衍生物中存在1 H -1,2,3-三唑环是造成这种活性的原因，可以用作抗糖尿病药。为了了解结合相互作用的方式和这类化合物的能量，对所有活性化合物进行了分子对接研究。