title: Synthesis of benzothiophene carboxamide derivatives and their pharmacological evaluation as potent antihypertriglyceridemic agents in rats.
abstract: Benzothiophene carboxamide derivatives of aminobenzophenone, aminopyridine, aminobenzimidazole, and aniline derivatives (compounds 1-9) were synthesized and compounds 3, 6, 7, 8, and 9 tested in vivo for their hypolipidemic activity. Compounds 1-8 were prepared adopting the fusion process at 130-150 degrees C between benzothiophene-2-carbonyl chloride and aminobenzophenones, aminopyridine, and anilines, respectively, and were obtained in high yield, while compound 9 was obtained from the reaction of benzothiophene acyl chloride with aminobenzimidazole in DMF at 160 degrees C. At a dose of 15 mg/kg body weight compounds 6, 7, and 9 significantly reduced plasma triglyceride levels in Triton WR-1339-induced hyperlipidemic rats in comparison to control rats. Furthermore, they significantly increased high-density lipoprotein levels. It is therefore reasonable to assume that compounds 6, 7, and 9 may have a promising potential in the treatment of hyperlipidemia and atherosclerosis.
authors.affiliation: Faculty of Pharmacy, Al-Zaytoonah Private University, Amman 11733, Jordan.
authors.forename: Ghassan
authors.initials: G
authors.lastname: Abu Sheikha
authors.forename: Buthina
authors.initials: B
authors.lastname: Hussin
authors.forename: Yusuf
authors.initials: Y
authors.lastname: Al-Hiari
authors.forename: Tariq
authors.initials: T
authors.lastname: Al-Qirim
authors.forename: Ghassan
authors.initials: G
authors.lastname: Shattat
mesh_terms: D000818:Animals; D015228:Hypertriglyceridemia / Q000188:drug therapy*; D000960:Hypolipidemic Agents / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000627:therapeutic use; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D021241:Spectrometry, Mass, Electrospray Ionization; D013055:Spectrophotometry, Infrared; D013876:Thiophenes / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000627:therapeutic use
chemical_list: D000960:Hypolipidemic Agents; D013876:Thiophenes; C088015:benzothiophene