Ao Imkongyanger, Richa Kikoleho, Lotha Tsenbeni N, Ao Ketiyala, Rudithongru Lemzila, Nakro Vevosa, Ritse Vimha, Namsa Nima D, Pankaj Pranay Punj, Sinha Upasana Bora, Jamir Latonglila
Department of Environmental Science, Nagaland University, Lumami, 798627, Nagaland, India.
Department of Biotechnology, St. Joseph University, Chumoukedima, 797115, Nagaland, India.
Endocr Metab Immune Disord Drug Targets. 2025;25(4):326-339. doi: 10.2174/0118715303287962240621053459.
Type 2 Diabetes Mellitus (T2DM) represents a significant and pressing worldwide health concern, necessitating the quest for enhanced antidiabetic pharmaceuticals. Guanidine derivatives, notably metformin and buformin, have emerged as pivotal therapeutic agents for T2DM management.
The present study introduces an efficient one-pot synthesis method for the production of symmetrical guanidine compounds and subsequently, their evaluation as potential T2DM agents.
This synthesis involves the reaction of isothiocyanates with secondary amines, employing an environmentally friendly and recyclable reagent, tetrabutylphosphonium tribromide (TBPTB). In order to understand the mechanics of ligand-protein interaction, ADME/Toxicity, and drug-likeliness aspects, in silico studies were incorporated.
An efficient and easy method for synthesis of guanidine compounds has been devised. Comprehensive assessment of the biological activity of the synthesized guanidine compounds, specifically in the context of T2DM, has been rigorously conducted.
Computational analyses have unveiled their substantial potential as promising antidiabetic agents. Results highlight the relevance of these compounds in the ongoing pursuit of novel therapeutic solutions for T2DM.
2型糖尿病(T2DM)是全球重大且紧迫的健康问题,因此需要寻求更有效的抗糖尿病药物。胍衍生物,尤其是二甲双胍和丁福明,已成为治疗T2DM的关键药物。
本研究介绍了一种高效的一锅法合成对称胍化合物的方法,并随后将其作为潜在的T2DM药物进行评估。
该合成方法涉及异硫氰酸酯与仲胺的反应,使用环境友好且可回收的试剂四丁基溴化鏻(TBPTB)。为了了解配体 - 蛋白质相互作用、ADME/毒性和药物相似性方面的机制,进行了计算机模拟研究。
已设计出一种高效且简便的胍化合物合成方法。已对合成的胍化合物的生物活性进行了全面评估,特别是在T2DM背景下。
计算分析揭示了它们作为有前景的抗糖尿病药物的巨大潜力。结果突出了这些化合物在持续寻求T2DM新型治疗方案中的相关性。