A series of 2-(substituted) phenyl and 2-indolyl quinoline derivatives (10a-l) was synthesized by an efficient microwave-assisted, trifluoroacetic acid-catalyzed, solvent-free method. Evaluation of the inhibitory activity led to the identification of two quinoline inhibitors of cholesterol esterase. 2-(1H-Indol-3-yl)-6-nitro-4-phenylquinoline (10l; IC50=1.98μM) was characterized as a mixed-type inhibitor with a pronounced competitive binding mode.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2014.01.081 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Mangiferin and EGCG Compounds Fight Against Hyperlipidemia by Promoting FFA Oxidation via AMPK/PPAR.
PPAR Res
December 2024
Yunnan Provincial Key Laboratory of Public Health and Biosafety & School of Public Health, Kunming Medical University, Kunming, Yunnan, China.
Hyperlipidemia is a critical risk factor for obesity, diabetes, cardiovascular diseases, and other chronic diseases. Our study was to determine the effects and mechanism of mangiferin (MF) and epigallocatechin gallate (EGCG) compounds on improving hyperlipidemia in HepG2 cells. HepG2 cells were treated with 0.
View Article and Find Full Text PDFEscalating Lipid Therapy After Achieving LDL-C <70 mg/dL With Moderate-Intensity Statins in High-Risk Patients.
Korean Circ J
November 2024
Division of Cardiology, Department of Internal Medicine, Yonsei University College of Medicine, Seoul, Korea.
Background And Objectives: Guidelines recommend target levels of low-density lipoprotein cholesterol (LDL-C) and intensive lipid-lowering therapy (LLT) in high-risk patients. However, the value of escalating LLT when the LDL-C targets are achieved with moderate-intensity statins is unknown. We aimed to evaluate the benefits of LLT escalation in this population.
View Article and Find Full Text PDFAssessment of dyslipidemia management in Turkey using a Delphi panel.
Sci Rep
December 2024
Department of Cardiology, Hacettepe University Faculty of Medicine, Ankara, Turkey.
This study evaluated the management of dyslipidemia in Turkey with the goal of understanding current diagnosis and treatment patterns, as well as identifying unmet needs in achieving effective low-density lipoprotein cholesterol (LDL-C) targets. Using a Delphi panel consisting of nine expert cardiologists, the study reveals key gaps in dyslipidemia management, particularly in the underutilization of combination therapies, such as statins and PCSK9 inhibitors, which are crucial for achieving LDL-C targets in high-risk patients. The findings indicate that while many patients with very high cardiovascular risk are diagnosed, a significant proportion do not receive optimal treatment to reach LDL-C levels recommended by European guidelines.
View Article and Find Full Text PDFBiomarkers and Seaweed-Based Nutritional Interventions in Metabolic Syndrome: A Comprehensive Review.
Mar Drugs
December 2024
Centre for Functional Ecology: Science for People & Planet, Marine Resources, Conservation and Technology-Marine Algae Lab, Department of Life Sciences, University of Coimbra, 3000-456 Coimbra, Portugal.
Metabolic Syndrome (MetS) is a complex, multifactorial condition characterized by risk factors such as abdominal obesity, insulin resistance, dyslipidemia and hypertension, which significantly contribute to the development of cardiovascular disease (CVD), the leading cause of death worldwide. Early identification and effective monitoring of MetS is crucial for preventing serious cardiovascular complications. This article provides a comprehensive overview of various biomarkers associated with MetS, including lipid profile markers (triglyceride/high-density lipoprotein cholesterol (TG/HDL-C) ratio and apolipoprotein B/apolipoprotein A1 (ApoB/ApoA1) ratio), inflammatory markers (interleukin 6 (IL-6), tumor necrosis factor alpha (TNF-α), plasminogen activator inhibitor type 1 (PAI-1), C-reactive protein (CRP), leptin/adiponectin ratio, omentin and fetuin-A/adiponectin ratio), oxidative stress markers (lipid peroxides, protein and nucleic acid oxidation, gamma-glutamyl transferase (GGT), uric acid) and microRNAs (miRNAs) such as miR-15a-5p, miR5-17-5p and miR-24-3p.
View Article and Find Full Text PDFExosome-derived miR-107 targeting caveolin-1 promotes gallstone progression by regulating the hepatobiliary cholesterol secretion pathway.
Biochem Pharmacol
December 2024
Department of Hepatobiliary Surgery, Shandong Provincial Hospital, Shandong University, Jinan 250021, Shandong Province, China. Electronic address:
Cholesterol gallstone is a disease with high incidence and quality of life. This study aimed to investigate the function of exosome-derived miRNA in gallstone formation and its related molecular mechanism. Exosomes were extracted and isolated from patients with gallbladder stones and age- and gender-matched healthy controls, and exosomal miRNA expression was compared between the two groups.
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!