title: Synthesis and pharmacological evaluation of novel substituted and unsubstituted N-(benzoylphenyl)-1H-indole-2-carboxamides as potent antihypertriglyceridemic agents.
abstract: The N-(benzoylphenyl)-1H-indole-2-carboxamide derivatives 1-6 were synthesized, and the lipid-lowering effects of two of these novel compounds were studied using hyperlipidemic rats as an experimental model. Treatment of ethyl-1H-indole-2-carboxylate with aminobenzophenones in the presence of sodium ethoxide and DMF, followed by purification using column chromatography, gave the target compounds in good yields. The tested animals were divided into control, hyperlipidemic, compounds 2-, 3- and bezafibrate-treated groups. At a dose of 15 mg/kg body weight, compounds 2, 3 and bezafibrate significantly reduced the elevated plasma triglyceride levels after 7 and 24 h. Furthermore, the high-density lipoprotein-cholesterol levels were remarkably increased in all treated groups after 7 and 24 h compared to the hyperlipidemic control group. However, only compounds 2- and 3-treated groups obviously showed a significant reduction in plasma total cholesterol levels after 24 h. It is therefore reasonable to assume that 2 and 3 may have a promising potential in the treatment of hyperlipidemia and coronary heart diseases.
authors.affiliation: Faculty of Pharmacy, Al-Zaytoonah Private University, Amman 11733, Jordan.
authors.forename: Moyad
authors.initials: M
authors.lastname: Shahwan
authors.forename: Ghassan
authors.initials: G
authors.lastname: Shattat
authors.forename: Tariq
authors.initials: T
authors.lastname: Al-Qirim
authors.forename: Ghassan Abu
authors.initials: GA
authors.lastname: Sheikha
authors.forename: Yusuf
authors.initials: Y
authors.lastname: Al-Hiari
authors.forename: Waseem
authors.initials: W
authors.lastname: El-Huneidi
authors.forename: Anan
authors.initials: A
authors.lastname: Jarab
authors.forename: Manal
authors.initials: M
authors.lastname: Al-Najdawi
mesh_terms: D000818:Animals; D001629:Bezafibrate / Q000627:therapeutic use; D002784:Cholesterol / Q000097:blood; D008076:Cholesterol, HDL / Q000097:blood; D008078:Cholesterol, LDL / Q000097:blood; D006949:Hyperlipidemias / Q000097:blood / Q000139:chemically induced / Q000188:drug therapy*; D000960:Hypolipidemic Agents / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000627:therapeutic use; D009682:Magnetic Resonance Spectroscopy / Q000379:methods; D008297:Male; D011092:Polyethylene Glycols; D051381:Rats; D017208:Rats, Wistar; D014280:Triglycerides / Q000097:blood
chemical_list: D008076:Cholesterol, HDL; D008078:Cholesterol, LDL; D000960:Hypolipidemic Agents; D014280:Triglycerides; D011092:Polyethylene Glycols; D002784:Cholesterol; C016811:tyloxapol; D001629:Bezafibrate