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Thiomorpholine Derivatives with Hypolipidemic and Antioxidant Activity
Ist Teil von
Archiv der Pharmazie (Weinheim), 2015-09, Vol.348 (9), p.629-634
Ort / Verlag
Germany: Blackwell Publishing Ltd
Erscheinungsjahr
2015
Link zum Volltext
Quelle
Wiley Online Library Journals Frontfile Complete
Beschreibungen/Notizen
A number of thiomorpholine derivatives that are structurally similar to some substituted morpholines possessing antioxidant and hypocholesterolemic activity were synthesized. The new compounds incorporate an antioxidant moiety as the thiomorpholine N‐substituent. The derivatives were found to inhibit the ferrous/ascorbate‐induced lipid peroxidation of microsomal membrane lipids, with IC50 values as low as 7.5 µΜ. In addition, these compounds demonstrate hypocholesterolemic and hypolipidemic action. The most active compound (5) decreases the triglyceride, total cholesterol, and low‐density lipoprotein levels in the plasma of Triton WR‐1339‐induced hyperlipidemic rats, by 80, 78, and 76%, respectively, at 56 mmol/kg (i.p.). They may also act as squalene synthase inhibitors. The above results indicate that the new molecules may be useful as leads for the design of novel compounds as potentially antiatherogenic factors.
Based on the already known lipid‐lowering and antioxidant action of morpholine derivatives, a series of substituted thiomorpholines were designed, further incorporating an antioxidant moiety as the N‐substituent. The new derivatives show considerable antioxidant potential with hypolipidemic activity and may also have combined squalene synthase inhibitory activity.