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Novel Quinoline- and Naphthalene-Incorporated Hydrazineylidene-Propenamide Analogues as Antidiabetic Agents: Design, Synthesis, and Computational Studies.
Pharmaceuticals (Basel)
December 2024
Department of Chemistry, Faculty of Science, Taibah University, Madinah 42353, Saudi Arabia.
Type 2 diabetes has become a significant global health challenge. Numerous drugs have been developed to treat the condition, either as standalone therapies or in combination when glycemic control cannot be achieved with a single medication. As existing treatments often come with limitations, there is an increasing focus on creating novel therapeutic agents that offer greater efficacy and fewer side effects to better address this widespread issue.
View Article and Find Full Text PDFTwo New α-Glucosidase Inhibitors from Haplophyllum tuberculatum: Inhibition Kinetics and Mechanistic Insights Through in Vitro and in Silico Approaches.
Chem Biodivers
December 2024
Natural & Medical Sciences Research Center, University of Nizwa, Nizwa, Oman.
Diabetes is a multifactorial global health disorder marked by unusually high plasma glucose levels, which can lead to serious consequences including diabetic neuropathy, kidney damage, retinopathy, and cardiovascular disease. One effective therapy approach for reducing hyperglycemia associated with type 2 diabetes is to target α-glucosidase, enzymes that catalyze starch breakdown in the intestine. In the current study, two new (1, 2) and nine known (3-11) compounds were isolated from the rutaceous plant Haplophyllum tuberculatum and characterized by extensive nuclear magnetic resonance spectroscopic techniques and high-resolution electrospray ionization mass spectrometry.
View Article and Find Full Text PDFDesign and synthesis of N-(3-cyanothiophen-2-yl)-2-phenoxyacetamide-based α-glucosidase inhibitors.
Bioorg Med Chem Lett
December 2024
School of Biological Science and Technology, University of Jinan, Jinan 250022, China. Electronic address:
This study investigates the design and synthesis of a series of novel selective α-glucosidase inhibitors based on N-(3-cyanothiophen-2-yl)-2-phenoxyacetamide framework, employing a bioisosterism strategy. Among the nineteen newly synthesized analogs, compound 4d9 demonstrated the highest α-glucosidase inhibitory potency (IC = 2.11 μM) when compared to the established inhibitors Acarbose (IC = 327.
View Article and Find Full Text PDFApigenin analogs as α-glucosidase inhibitors: Molecular docking, biochemical, enzyme kinetic, and an in vivo mouse model study.
Bioorg Chem
December 2024
Department of Gastroenterology, Zhongnan Hospital of Wuhan University, Wuhan 430071, China; Hubei Provincial Clinical Research Center for Intestinal and Colorectal Diseases, Hubei Key Laboratory of Intestinal and Colorectal Diseases, Wuhan 430071, China. Electronic address:
Due to the high incidence of diabetes and its associated complications, diabetes is widely recognized as a serious global health problem. In diabetes treatment strategies, targeting α-glucosidase, a key carbohydratehydrolyzing enzyme, has emerged as a highly regarded approach. To develop novel α-glucosidase inhibitors, we successfully synthesized a series of apigenin analogs, collectively referred to as H1-H27 compounds and examined their inhibitory effects on α-glucosidase activity.
View Article and Find Full Text PDFSynthesis of arylated tetrahydrobenzo[]quinoline-3-carbonitrile derivatives as potential hits for treatment of diabetes.
Future Med Chem
December 2024
H. E. J. Research Institute of Chemistry, International Center for Chemical & Biological Sciences, University of Karachi, Karachi, 75270, Pakistan.
Quinoline scaffolds are serving as the core structure for numerous antifungal, analgesic, antipyretic, anti-inflammatory drugs as well as have also been investigated for their potential antidiabetic properties. Though further exploration is required in this area as the current antidiabetic agents, such as acarbose, miglitol and voglibose, are associated with several adverse side effects. In this context, arylated tetrahydrobenzo[]quinoline-3-carbonitrile derivatives were designed and evaluated as potential antidiabetic agents.
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