Search results for "Azetidines"
showing 6 items of 26 documents
Novel Penicillin-Type Analogues Bearing a Variable Substituted 2-Azetidinone Ring at Position 6: Synthesis and Biological Evaluation
2015
The synthesis and the biological activity of novel semi-synthetic β-lactam compounds containing an azetidinone moiety joined to the amino-nitrogen of the (+)-6-aminopenicillanic acid (6-APA) as new antibacterial agents is reported. The synthesized compounds were screened for their in vitro antimicrobial activity against a panel of Gram positive and Gram negative pathogens and environmental bacteria. Tested compounds displayed good antimicrobial activity against all tested Gram positive bacteria and for Staphylococcus aureus and Staphylococcus epidermidis antimicrobial activity resulted higher than that of the reference antibiotic. Additionally, in vitro cytotoxic screening was also carried …
Lipid-Altering Efficacy of Ezetimibe/Simvastatin 10/20 mg Compared to Rosuvastatin 10 mg in High-Risk Patients with and without Type 2 Diabetes Melli…
2010
AIMS: This post hoc analysis compared the effects of switching to ezetimibe/simvastatin 10/20 mg (EZE/SIMVA) or rosuvastatin 10 mg (ROSUVA) in uncontrolled high-risk hypercholesterolemic patients with/without type 2 diabetes mellitus (T2DM) despite statin monotherapy. METHODS: Patients (n = 618) at high risk for coronary vascular disease with elevated LDL-C ≥100 and ≤190 mg/dL despite use of statins were randomized 1:1 to double-blind EZE/SIMVA 10/20 mg or ROSUVA 10 mg for 6 weeks. Patients were classified as having T2DM based on ≥1 of the following: diagnosis of T2DM, antidiabetic medication, or FPG ≥126 mg/dL. This analysis evaluated percent changes from baseline in lipids among patients …
Effects of statins, fibrates, rosuvastatin, and ezetimibe beyond cholesterol: the modulation of LDL size and subclasses in high-risk patients.
2007
Increasing evidence suggests that the quality-rather than just the quantity-of low-density lipoproteins (LDLs) exerts a great influence on cardiovascular risk. LDLs comprise multiple subclasses with discrete size and density, and different physicochemical composition, metabolic behaviors, and atherogenicity. Individuals generally cluster into 2 broad subgroups. Most have a predominance of large LDLs, and some have a higher proportion of small particles. Small, dense LDLs are good predictors of cardiovascular events and progression of coronary artery disease. Their predominance has been accepted as an emerging cardiovascular risk factor by the National Cholesterol Education Program Adult Tre…
The effects of ezetimibe on LDL-cholesterol: quantitative or qualitative changes ?
2009
Ezetimibe represents the first of a new class of agents, the cholesterol absorption inhibitors, able to reduce low-density lipoproteins (LDL)-cholesterol by 15-25% from baseline in monotherapy and on top of statins and fibrates. To-date all the data regarding the efficacy of ezetimibe comes from the studies of its lipid-lowering power. Yet, recent findings from the ENHANCE study on atherosclerosis progression showed that the addition of ezetimibe to simvastatin in patients with heterozygous familial hypercholesterolemia did not affect the mean change in carotid intima-media thickness, although a significant reduction in LDL-cholesterol levels was present. Therefore, we cannot exclude that e…
Adipokines and Lipoproteins: Modulation by Antihyperglycemic and Hypolipidemic Agents
2014
Abstract Adipose tissue is an endocrine organ that secretes a number of hormones and metabolically active substances that impact energy metabolism and insulin sensitivity. These inflammatory markers are collectively referred to as adipocytokines, or adipokines. Adipose tissue's functional capacity and metabolic activity vary among individuals, thus partly explaining the incomplete overlap between obesity and the metabolic syndrome. The functional failure of adipose tissues results in changed energy delivery and impaired glucose consumption, triggering self-regulatory mechanisms to maintain homeostasis. Antihyperglycemic, hypolipidemic, antiobesity, and angiotensin II receptor blocker drugs …
The effect of ezetimibe on NAFLD
2015
NAFLD has become the most common liver disorder in countries, where obesity, type 2 diabetes mellitus, dyslipidemia, and metabolic syndrome are common. The strong association between these conditions and the risk of cardiovascular disease make treatment crucial. Possible interventions for NAFLD target excess body weight, insulin resistance, inflammation, oxidative stress or intestinal lipid absorption. Administration of combination therapy with a statin plus ezetimibe, associated with lifestyle changes, may represent an effective strategy because of the strong reduction in low-density lipoprotein cholesterol levels. Combination therapy is often more effective, especially when complementary …