title: Synthesis of novel N-(2-hydroxy-2-p-tolylethyl)-amide and N-(2-oxo-2-p-tolylethyl)-amide derivatives and their antidyslipidemic and antioxidant activity.
abstract: In continuation of our drug discovery program on metabolic diseases, we identified an alkaloidal amide, that is, Aegeline (V) from the plant Aegle marmelos leaves as a dual acting agent (antihyperlipidemic and antihyperglycemic). We therefore synthesized a series of alkaloidal amides [N-(2-hydroxy-2-p-tolylethyl)-amides and N-(2-oxo-2-p-tolylethyl)-amide derivatives] related to Aegeline and screened for their in vivo antihyperlipidemic activity in Triton induced hyperlipidemia model. The synthetic compounds 4, 17 and 20 showed equipotent activity to the natural product, that is, Aegeline (V). These compounds also showed strong antioxidant activity, which support their antihyperlipidemic activity. Compound 12 showed better antihyperlipidemic and antioxidant profile than the natural product V.
authors.affiliation: Medicinal and Process Chemistry Division, Central Drug Research Institute (CSIR), Lucknow 226 001, UP, India. t_narendra@cdri.res.in
authors.forename: T
authors.initials: T
authors.lastname: Narender
authors.forename: K
authors.initials: K
authors.lastname: Rajendar
authors.forename: S
authors.initials: S
authors.lastname: Sarkar
authors.forename: V K
authors.initials: VK
authors.lastname: Singh
authors.forename: Upma
authors.initials: U
authors.lastname: Chaturvedi
authors.forename: A K
authors.initials: AK
authors.lastname: Khanna
authors.forename: G
authors.initials: G
authors.lastname: Bhatia
mesh_terms: D000818:Animals; D000975:Antioxidants / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000960:Hypolipidemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008297:Male; D051381:Rats; D014050:Toluene / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000975:Antioxidants; D000960:Hypolipidemic Agents; D014050:Toluene