Synthesis and in Vivo Lipid-Lowering Activity of Novel Imidazoles-5-carboxamide Derivatives in Triton-WR-1339-Induced Hyperlipidemic Wistar Rats
Autor: | 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, Suhair H Jasim |
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Rok vydání: | 2018 |
Předmět: |
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 |
Zdroj: | Chemical and Pharmaceutical Bulletin. 66:953-958 |
ISSN: | 1347-5223 0009-2363 |
DOI: | 10.1248/cpb.c18-00346 |
Popis: | 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 |
Databáze: | OpenAIRE |
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