Pasha Anam Rubbab, Ullah Saeed, Khan Ajmal, Halim Sobia Ahsan, Hussain Javid, Rehman Tanzila, Talib Rimsha, Alharthy Rima D, Kashtoh Hamdy, Abdellattif Magda H, Al-Harrasi Ahmed, Shafiq Zahid
Institute of Chemical Sciences, Bahauddin Zakariya University Multan-60800 Pakistan
Natural and Medical Sciences Research Centre, University of Nizwa P.O. Box 33, PC 616, Birkat Al Mauz Nizwa Sultanate of Oman
RSC Adv. 2024 Sep 16;14(40):29288-29300. doi: 10.1039/d4ra05767h. eCollection 2024 Sep 12.
Diabetes mellitus has become a major global health burden because of several related consequences, including heart disease, retinopathy, cataracts, metabolic syndrome, collapsed renal function, and blindness. In the recent study, thirty Schiff base derivatives of 1,3-diphenylurea were synthesized and their anti-diabetic activity was evaluated by targeting α-glucosidase. The compounds exhibited an overwhelming inhibitory potential for α-glucosidase with higher potency ranging from 2.49-37.16 μM. The most effective compound, 5h, showed competitive inhibition of α-glucosidase ( = 3.96 ± 0.0048 μM) in the kinetic analysis and strong binding interactions with key residues α-glucosidase in docking analysis, indicating its potential for better glycemic control in diabetes patients.
由于包括心脏病、视网膜病变、白内障、代谢综合征、肾功能衰竭和失明在内的多种相关后果，糖尿病已成为全球主要的健康负担。在最近的研究中，合成了30种1,3 - 二苯基脲席夫碱衍生物，并通过靶向α - 葡萄糖苷酶评估了它们的抗糖尿病活性。这些化合物对α - 葡萄糖苷酶表现出压倒性的抑制潜力，效价较高，范围为2.49 - 37.16 μM。最有效的化合物5h在动力学分析中显示出对α - 葡萄糖苷酶的竞争性抑制（ = 3.96 ± 0.0048 μM），并且在对接分析中与α - 葡萄糖苷酶的关键残基有强烈的结合相互作用，表明其在糖尿病患者中实现更好血糖控制的潜力。
