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anti-diabetic and anti-lipidemic evaluations of an excellent synthetic α-glucosidase inhibitor with dihydropyrano[3,2-c]quinoline skeleton.
J Diabetes Metab Disord
December 2024
Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran.
Objectives: The assay is a key step in the development of a new bioactive compound as a lead drug structure. Based on importance of α-glucosidase inhibitors in the control of blood glucose level (BGL) in diabetes, in the present work, 3-amino-1-(4-chlorophenyl)-12-oxo-11,12-dihydro-1-benzo[]pyrano[3,2-]quinoline-2-carbonitrile () that showed excellent inhibitory activity on the yeast form of α-glucosidase was selected for anti-diabetic assay.
Methods: The anti-diabetic and anti-lipidemic effects of this synthetic compound were evaluated using by a streptozotocin (STZ)-induced diabetic Wistar rat model.
Triazole scaffold-based DPP-IV Inhibitors for the management of Type-II Diabetes Mellitus: Insight into Molecular Docking and SAR.
Curr Top Med Chem
October 2024
Department of Pharmacology, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi-110062, India.
Diabetes mellitus, characterized as a chronic metabolic disorder or a polygenic syndrome; is increasing at a very fast pace among every group of the population worldwide. It arises due to the inability of the body to produce enough insulin (the hormone responsible for controlling blood sugar levels) or inability to utilize the insulin, leading to hyperglycaemic condition, which, if left uncontrolled gives rise to chronic microvascular and macrovascular complications like retinopathy, neuropathy, nephropathy, coronary artery disease, cognitive impairment, etc. Several therapeutic approaches are available for the treatment of diabetes; among which dipeptidyl peptidase (DPP-IV) inhibitors (gliptins) hold a significant place.
View Article and Find Full Text PDFDiscovery of novel dihydro-pyrimidine hybrids: insight into the design, synthesis, biological evaluation and absorption, distribution, metabolism and excretion studies.
Future Med Chem
October 2024
Synthetic & Natural Products Discovery (SNPD) Laboratory, Department of Chemistry, Government College Women University, Faisalabad, 38000, Pakistan.
By keeping in aspects, the pharmacological potential of heterocyclic compounds, pyrimidine-based compounds were designed, synthesized and evaluated for α-amylase inhibitory potential. Five new series 1a-l, 2a-d, 3a-d, 4a-d and 5a-d of 1,2,3,4-tetrahydroprimidine-5-carboxylate derivatives were designed by method by taking Alogliptin as reference compound. Here in we describe synthesis and characterization of compounds as potential α-amylase inhibitor.
View Article and Find Full Text PDFMolecular Mechanisms Underlying the Therapeutic Potential of Plant-Based α-Amylase Inhibitors for Hyperglycemic Control in Diabetes.
Curr Diabetes Rev
July 2024
Chitkara College of Pharmacy, Chitkara University, 140401, Punjab, India.
Background: Diabetes mellitus (DM), arising from pancreatic β-cell dysfunction and disrupted alpha-amylase secretion, manifests as hyperglycemia. Synthetic inhibitors of alphaamylase like acarbose manage glucose but pose adverse effects, prompting interest in plantderived alternatives rich in antioxidants and anti-inflammatory properties.
Objective: The current review investigates plant-based alpha-amylase inhibitors, exploring their potential therapeutic roles in managing DM.
and evaluations of a synthetic pyrano[3,2-c]quinoline derivative as a potent anti-diabetic agent.
J Diabetes Metab Disord
June 2024
Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran.
Background: The assessment of a novel compound is a pivotal step in the development of a new drug. In this study, we selected 1-(2-bromophenyl)-1,11-dihydro-3H-benzo[h]pyrano[3,2-c]quinoline-3,12(2H)-dione (), identified as an exemplary α-glucosidase inhibitor in preliminary in vitro assays, for further evaluation in an anti-diabetic context.
Methods: The anti-diabetic effect of was assessed using a streptozotocin (STZ)-induced diabetic Wistar rat model.
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