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SYNTHESIS AND HYPOLIPIDEMIC ACTIVITY OF ASARONE ANALOGS IN MALE AND FEMALE RATS |
Bożena Łozowicka 1, Janusz Popławski 1, Alina Dubis 1, Jacek Cybulski 2, Zdzisław Chilmonczyk 1,3, Kazimierz Kita 4, Sławomir Filipek 5 |
1. University of Białystok, Institute of Chemistry, Hurtowa 1, Białystok 15-399, Poland |
Abstract |
A series of alpha-asarone analogs were synthesized and tested for hypolipidemic activity (against Clofibrate as a reference drug) in male and female rats. Compounds 5-((1E)-but-1-enyl)-1,2,3-trimethoxybenzene (7), 5-((1E)-okt-1-enyl)-1,2,3-trimethoxybenzene (11), 2,6-dimethoxy-4-[(1E)-prop-1-enyl]phenyl nicotinate (21), 2,6-dimethoxy-4-[(1E)-pent-1-enyl]phenyl nicotinate (22) and {2,6-dimethoxy-4-[(1E)-pent-1-enyl]phenoxy}-4-oxobutanoic acid (24) reduced the total cholesterol, LDL cholesterol and increased the HDL cholesterol in male rats. Furthermore, compounds (11), (22) and (24) decreased triglyceride levels. Interestingly, compound (22) reduced the total cholesterol, LDL cholesterol and increased the HDL cholesterol also in female population. Thus, compound (22) 2,6-dimethoxy-4-[(1E)-pent-1-enyl]phenyl nicotinate may be considered as a good candidate for effective hypolipidemic drug. QSAR studies were conducted to examine the influence of structural properties on the compounds hypolipidemic activity. |
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Presentation: Poster at V Multidyscyplinarna Konferencja Nauki o Leku, by Bożena ŁozowickaSee On-line Journal of V Multidyscyplinarna Konferencja Nauki o Leku Submitted: 2006-03-20 11:19 Revised: 2009-06-07 00:44 |