Synthesis and in vivo anti-hyperlipidemic activity of novel n-benzoylphenyl-2-furamide derivatives in Wistar rats

Purpose: To synthesize and evaluate the anti-hyperlipidemic activity of a novel series of N- (benzoylphenyl)-2-furamides (3a, 3b, 4a, 4b and 4c).Methods: Compounds (3a, 3b, 4a, 4b and 4c) were successfully synthesized by reacting activated furan-2-carbonyl-chloride derivatives with aminobenzophenones at 60 °C for 36 h. Hyperlipidemia was induced in overnight fasted rats by intraperitoneal administration of Triton WR-1339 (300 mg/kg). to overnight fasted rats. The rats were divided into six groups: control, hyperlipidemic, hyperlipidemic plus compounds 3b, 4b, 4c, and hyperlipidemic plus bezafibrate-treated. Eighteen hours later, blood samples were collected and plasma lipid profile determined using enzymatic methods.Results: At a dose of 15 mg/kg body weight, the elevated plasma triglyceride (TG) levels, total cholesterol (TC) and low density lipoprotein cholesterol (LDL-C) levels were significantly reduced by compounds 4b (p < 0.001) and 4c (p < 0.0001) 18 h later, compared to the hyperlipidemic group. Furthermore, compounds 4b and 4c significantly increased high density lipoprotein cholesterol (HDL-C) levels by 29 and 34 %, respectively.Conclusion: The findings indicate the high potency of N-(benzolphenyl)-2-furamides (4b and 4c) as lipid-lowering agents. Thus, these compounds 4b and 4c may used as lead compounds for the development of new derivatives and agents for targeting dyslipidemia and cardiovascular diseases.Keywords: Triton WR-1339-induced hyperlipidemic rats, N-(benzoylphenyl)-2-furamides, Lipid-lowering activity, Cardiovascular disease, Synthesi

Synthesis and In Vivo Hypolipidemic Effect of Some N-(Benzoylphenyl)-Carboxamide Derivatives in Triton WR-1339-Induced Hyperlipidemic Rats

A series of N-(benzoylphenyl)-carboxamide derivatives (2a, 2b, 3a, 3b, 4a, 4b, 5a, 5b, 6a and 6b) was prepared with good yields by reacting the corresponding carbonyl chlorides with aminobenzophenones at room temperature. This was followed by evaluating the hypotriglyceridemic and hypocholesterolemic effects of 3b, 5a and 5b. Triton WR-1339 (300 mg/kg) was intraperitoneally administered to overnight-fasted rats to induce hyperlipidemia. Rats were divided into six groups: control, hyperlipidemic, hyperlipidemic plus compounds 3b, 5a and 5b and hyperlipidemic plus bezafibrate. Results showed that after 18 h of treatment at a dose of 15 mg/kg body weight of each of the test compounds, the elevated plasma levels of triglycerides (TG) and total cholesterol (TC) were significantly lowered by compounds 5b and 3b (p < 0.001) and by 5a (p < 0.0001), compared to the hyperlipidemic control group. Compounds 3b and 5a significantly increased levels of high-density lipoprotein cholesterol (HDL-C) by 58 and 71%, respectively. In addition, compounds 3b and 5a caused significant reduction (p < 0.0001) of low-density lipoprotein cholesterol (LDL-C) levels compared to the control group. These results suggest a promising potential for compounds 3b, 5a and 5b as lipid-lowering agents, which may contribute to reducing the risk of atherosclerosis and cardiovascular disease

Synthesis and Anti-Hyperlipidemic Evaluation of N‑(Benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide Derivatives in Triton WR-1339-Induced Hyperlipidemic Rats

The lipid-lowering activity of a series of novel N-(benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide derivatives has been studied in Triton WR-1339-induced hyperlipidemia in rats. The test animals were divided into four groups: control, hyperlipidemic, compound + 4% DMSO [C1: N-(2-benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide (1), C2: N-(3-benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide (2), C3: N-(4-benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide (3)]-treated and bezafibrate (BF)-treated. At a dose of 15 mg/Kg body weight, compounds 2, 3 and BF significantly reduced elevated plasma triglycerodes levels after 12 h. Moreover, high density lipoprotein-cholesterol levels were significantly increased in all treated groups after 12 h compared to the hyperlipidemic control group, except for C1 which was inactive. In sum, it may be stated that the results of the present study demonstrated new properties of some N-(benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide derivatives as potent lipid lowering agents and these beneficial activities may contribute to their cardioprotective and antiatherosclerotic role

Blood pressure, heart rate and CNS stimulant medication use in children with and without ADHD: analysis of NHANES data

It is estimated that 2-3% of children in the US have hypertension (HTN) and 8% of children ages 4-17 carry the diagnosis of Attention Deficit Hyperactivity Disorder (ADHD). The prevalence of HTN and cardiovascular (CV) risk factors in children with ADHD on CNS stimulant treatment (stimulants) compared to no treatment and compared to their healthy counterparts is not well described. Using NHANES data, we examined demographic, BP and CV risk factors of 4,907 children aged 12-18 years with and without the diagnosis of ADHD, and further examined the CV risk in a subgroup of ADHD patients on stimulants. 383 (10.7%) children were reported to have ADHD; of whom 111 (3.4%) were on stimulants. Children with ADHD on stimulants were significantly younger, male, and white compared to those with ADHD not on medication and those without ADHD. BMI, eGFR, cholesterol, the prevalence of albuminuria and poverty were not significantly different between the three groups. 160 (2.7%) had BP in the hypertensive and 637 (12.4%) in the prehypertensive range. The prevalence of elevated BP (HTN and/or pre-HTN range) was not different between children with ADHD on stimulants compared to ADHD without medication and those without ADHD. Heart Rate (HR) was significantly higher in the ADHD group on stimulants vs. the groups ADHD on no stimulants and without ADHD. When the relationship between stimulants and the risk of abnormal BP was examined, there was a significant interaction between having BP in the HTN range and sex. After adjusting for BMI, race and age, females with ADHD on stimulants tended to be older and had significantly more BP in the hypertensive range. On the other hand, males were more likely to be of a white race and older, but not hypertensive.Children with ADHD on stimulants have significantly higher HR than children with ADHD on no stimulants and children without ADHD. On the other hand, the prevalence of abnormal BP classification is comparable between the three groups

7-(3-Chlorophenylamino)-1-cyclopropyl-6-fluoro-8-nitro-4-oxo-1,4-dihydroquinoline-3-carboxylic Acid

7-(3-Chlorophenylamino)-1-cyclopropyl-6-fluoro-8-nitro-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid (2) was prepared and fully characterized by NMR, IR, and MS. Compound 2 exhibited good antibacterial activity against gram-positive standard and resistant strains