1. Synthesis and in Vivo Lipid-Lowering Activity of Novel Imidazoles-5-carboxamide Derivatives in Triton-WR-1339-Induced Hyperlipidemic Wistar Rats
- Author
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Ghassan Abu Sheikha, Mustafa S Aboumair, Samah A. Ata, Dima A. Sabbah, Majdi M. Bkhaitan, Tariq Al-Qirim, Kamal Sweidan, Ghassan Shattat, Samah A Ala, Haneen M Abuzaid, and Suhair H Jasim
- Subjects
Male ,medicine.drug_class ,medicine.medical_treatment ,Intraperitoneal injection ,Hyperlipidemias ,Carboxamide ,Pharmacology ,01 natural sciences ,Chloride ,Polyethylene Glycols ,chemistry.chemical_compound ,Pharmacokinetics ,In vivo ,Drug Discovery ,medicine ,Animals ,Rats, Wistar ,Intubation, Gastrointestinal ,Hypolipidemic Agents ,Bezafibrate ,Molecular Structure ,Triglyceride ,010405 organic chemistry ,Imidazoles ,General Chemistry ,General Medicine ,Lipids ,Rats ,0104 chemical sciences ,010404 medicinal & biomolecular chemistry ,Solubility ,chemistry ,Lipoproteins, HDL ,medicine.drug ,Lipoprotein - Abstract
A new series of imidazole-5-carboxamide derivatives were prepared and tested for their anti-hyperlipidemic activity in Triton-WR-1339-induced hyperlipidemic Wistar rats. The purpose of this research was to improve benzophenone carboxamides water solubility maintaining at the same time the antihyperlipidemic activity. Compounds 4, 6, 10, and 11 were synthesized through a coupling reaction between imidazoles-5-carbonyl chloride and amino benzophenones. The tested animals (n=48) were divided into six groups: the first group (hyperlipidemic control group; HCG) received an intraperitoneal injection (i.p.) of (300 mg/kg) Triton WR-1339. The second group received i.p. injection of Triton WR-1339 followed by an intra-gastric administration of bezafibrate (100 mg/kg) (bezafibrate; BF). The third, fourth, fifth, and sixth groups received i.p. injection of Triton WR-1339 followed by an intra-gastric administration of (30 mg/kg) of compounds 4, 6, 10, and 11, respectively. At a dose of 30 mg/kg body weight compounds 4, 6, 10, and 11 significantly (p
- Published
- 2018
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