Synthesis and Pharmacological Evaluation of Novel Unsubstituted Indole-Anthraquinone Carboxamide Derivatives as Potent Antihyperlipidemic Agents
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Manal Al-Najdawi
,
Yusuf Hiari
Five novel derivatives of N-(9,10-dihydro-9,10-dioxoanthracenyl)-1H-indole-2-carboxamide were synthesized and their lipid-lowering effects studied in hyperlipidemic rats. Fusion of the anthraquinone derivatives at high temperature with 5-indole-2-carbonyl chloride, followed by recrystallization from chloroform=methanol gave the desired compounds in excellent yields. Compounds 1 to 5 at a non-toxic dose (1 ml of 57 mM solutions) and bezafibrate as positive control were administered to rats that were hyperlipidemic due to treatment with Triton WR-1339. A decrease in the plasma levels of triglyceride (TG) and low-density lipoprotein-cholesterol (LDL-C) and an increase in the plasma level of high-density lipoprotein-cholesterol (HDL-C) were observed with compounds 1, 3, 4, and 5. Compounds 1, 4, and 5 significantly reduced total cholesterol (TC) levels as well. These compounds may provide agents for targeting dyslipidemia and cardiovascular disease.
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Articles in the same Issue
- Anti-Inflammatory Activity of Selected Plants from Saudi Arabia
- Propolis from Northern California and Oregon: Chemical Composition, Botanical Origin, and Content of Allergens
- Synthesis and Pharmacological Evaluation of Novel Unsubstituted Indole-Anthraquinone Carboxamide Derivatives as Potent Antihyperlipidemic Agents
- Anthraquinones from Vismia mexicana
- Vascular and Antioxidant Effects of an Aqueous Mentha cordifolia Extract in Experimental NG-Nitro-L-arginine Methyl Ester-Induced Hypertension
- Bioguided Identification of Antifungal and Antiproliferative Compounds from the Brazilian Orchid Miltonia flavescens Lindl.
- Interspecific Competition between Microcystis aeruginosa and Anabaena flos-aquae from Taihu Lake, China
- Influence of Culture Conditions on the Biotransformation of (+)-Limonene by Aspergillus niger
- Low-Dose Radiation Suppresses Pokemon Expression under Hypoxic Conditions
- Polyamines in Cell Walls of Chlorococcalean Microalgae
- Identification of an Endoplasmic Reticulum Membrane Protein Interacting with DNA Polymerase Beta by a Yeast Two-Hybrid Screen
