Novel C-aryl glucoside SGLT2 inhibitors containing 1,3,4-thiadiazole moieties were designed and synthesized. Among the compounds tested, biaryl-type compounds containing pyrazine 59, 2-furan 61, and 3-thiophene 71 showed the best in vitro inhibitory activities to date (IC(50) = 3.51-7.03 nM) against SGLT2. A selected compound 61, demonstrated reasonable blood glucose-lowering effects, indicating that the information obtained from the SAR studies in this 1,3,4-thiadiazolylmethylphenyl glucoside series might help to design more active SGLT2 inhibitors that are structurally related.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmc.2010.01.073 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
New Insights into the Role of SGLT-2 Inhibitors in the Prevention of Dementia.
Neurol Int
December 2024
School of Medicine, Chung Shan Medical University, Taichung 40201, Taiwan.
Diabetes mellitus (DM) is a chronic disease associated with numerous complications, including cardiovascular diseases, nephropathy, and neuropathy. Sodium-glucose cotransporter 2 (SGLT-2) inhibitors, a class of novel antidiabetic agents, have demonstrated promising therapeutic effects beyond glycemic control, with potential benefits extending to the cardiovascular and renal systems. Recently, research has increasingly focused on exploring the potential role of SGLT-2 inhibitors in preventing dementia.
View Article and Find Full Text PDFEffectiveness of add-on therapy with SGLT2 inhibitors or GLP-1 receptor agonists in adults with type 1 diabetes: A prospective DPV registry study.
Diabetes Obes Metab
December 2024
German Center for Diabetes Research (DZD), Munich-Neuherberg, Germany.
Commentary on the 2021 update of the KDIGO clinical practice guideline for management of blood pressure in chronic kidney disease.
Nephrology (Carlton)
January 2025
Forward Thinking Design, Sydney, New South Wales, Australia.
The 2021 KDIGO clinical practice guideline for the management of blood pressure (BP) in chronic kidney disease (CKD) provided significant practice-changing recommendations for the care of both adult and paediatric CKD patients not receiving dialysis. The purpose of this review is to contextualise these recommendations and evaluate their applicability to the Australian and New Zealand context. Key updates presented in this guideline relate to measurement techniques, with a strong recommendation for standardised office BP measurement, as opposed to routine office BP measurement.
View Article and Find Full Text PDFAssessing the benefit-risk profile of newer glucose-lowering drugs: A systematic review and network meta-analysis of randomized outcome trials.
Diabetes Obes Metab
December 2024
The Center for Health AI and Synthesis of Evidence (CHASE), University of Pennsylvania, Philadelphia, Pennsylvania, USA.
Aim: To comprehensively evaluate the benefits and risks of glucagon-like peptide-1 receptor agonists (GLP-1RA), dipeptidyl peptidase 4 inhibitors (DPP4i), and sodium-glucose cotransporter 2 inhibitors (SGLT2i).
Materials And Methods: A systematic search of PubMed, EMBASE, and Cochrane Central Register of Controlled Trials (CENTRAL) from inception to November 2023 to identify randomized cardiovascular and kidney outcome trials that enrolled adults with type 2 diabetes, heart failure, or chronic kidney disease and compared DPP4i, GLP-1RAs, or SGLT2i to placebo. Twenty-one outcomes (e.
Type 2 diabetes mellitus (T2DM) is a chronic metabolic disorder characterized by hyperglycemia, insulin resistance, and decreased insulin secretion. With its rising global prevalence, effective management strategies are critical to reducing morbidity and mortality. This systematic review compares the efficacy, safety, and long-term outcomes of four major pharmacological treatments for T2DM: sodium-glucose cotransporter-2 (SGLT2) inhibitors, dipeptidyl peptidase-4 (DPP-4) inhibitors, metformin, and insulin.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!