title: Hybrid benzofuran-bisindole derivatives: new prototypes with promising anti-hyperlipidemic activities.
abstract: A series of different benzofuran-bisindole hybrids were synthesized and evaluated in vitro for their antioxidant and in vivo for antidyslipidemic activity in triton WR-1339 induced hyperlipidemic rats. Among the series, compounds 4a, 4c, 4h and 4j showed significant decrease in plasma levels of total cholesterol (TC), phospholipids (PL) and triglycerides (TG) followed by increase in post heparin lipolytic activity (PHLA). In addition, the active hybrids possessed moderate antioxidant properties and increased the plasma lecithin cholesterol acyltransferase (LCAT) activity, which plays a key role in lipoprotein metabolism contributing to an increased level of HDL-C in serum. These results indicate that these hybrids constitute novel prototypes for the management of dyslipidemia.
authors: Medicinal and Process Chemistry Division, CSIR - Central Drug Research Institute, Lucknow 226 001, Uttar Pradesh, India. Electronic address: sashidhar123@gmail.com.
authors: Koneni V
authors: KV
authors: Sashidhara
authors: Ram K
authors: RK
authors: Modukuri
authors: Ravi
authors: R
authors: Sonkar
authors: K Bhaskara
authors: KB
authors: Rao
authors: Gitika
authors: G
authors: Bhatia
mesh_terms: D000818:Animals; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001572:Benzofurans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002784:Cholesterol / Q000097:blood; D004789:Enzyme Activation / Q000187:drug effects; D000960:Hypolipidemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008066:Lipolysis / Q000187:drug effects; D008297:Male; D015394:Molecular Structure; D007862:Phosphatidylcholine-Sterol O-Acyltransferase / Q000097:blood; D010743:Phospholipids / Q000097:blood; D051381:Rats; D014280:Triglycerides / Q000097:blood
chemical_list: D000975:Antioxidants; D001572:Benzofurans; D000960:Hypolipidemic Agents; D007211:Indoles; D010743:Phospholipids; D014280:Triglycerides; D002784:Cholesterol; D007862:Phosphatidylcholine-Sterol O-Acyltransferase; C105430:benzofuran
keywords: Benzofuran–bisindole; LCAT activity; Lipid lowering activity; Lipoprotein metabolism; Triton model