کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1394095 | 1501136 | 2014 | 10 صفحه PDF | دانلود رایگان |

• We have synthesized fifteen new N-acyl-1-amino-2-alcohols, related to Aegeline.
• All were screened for lipid lowering, LDL-oxidation and antioxidant activity.
• Compounds 3, 11, 13 showed drug like lipid lowering, LDL-oxidation and antioxidant activity.
As a part of our drug discovery program, we identified an alkaloidal amide i.e. Aegeline (V) isolated from the leaves of Aegle marmelos as a dual acting agent (antihyperlipidemic and antihyperglycemic). In continuation of this program, we synthesized new N-acyl-1-amino-2-alcohols (N-acrylated-1-amino-2-phenylethanol and N-acylated-1-amino-3-aryloxypropanols) via Ritter reaction and screened for their in-vivo antihyperlipdemic activity in Triton induced hyperlipidemia model, LDL-oxidation and antioxidant activity. Compounds 3, 11 and 13 showed good antihyperlipidemic activity, LDL-oxidation as well as antioxidant activity and comparable activity with marketed antidyslipidemic drug.
New N-acyl-1-amino-2-alcohols (3 and 8–21) were synthesized and evaluated their antihyperlipdemic, LDL-oxidation and antioxidant activity. Compounds 3, 11 and 13 showed comparable activity with marketed antidyslipidemic drug.Figure optionsDownload as PowerPoint slide
Journal: European Journal of Medicinal Chemistry - Volume 80, 10 June 2014, Pages 135–144