Nitric oxide releasing morpholine derivatives as hypolipidemic and antioxidant agents.
The synthesis and evaluation of activity of some nitric acid esters of substituted morpholines are presented. All compounds inhibit lipid peroxidation and reduce cholesterol (20-63%) and triglyceride (37-85%) plasma levels. The more potent NO donors 14 and 17 specifically reduce low-density lipoprotein (LDL). These data indicate that proper structural modifications to the hypolipidemic and antioxidant morpholines enabling NO production, besides preserving or enhancing the above activities, offer a remarkable reduction of LDL, considered advantageous for antiatheromatic agents.
Chrysselis
Michael C
MC
Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, Thessaloniki 54 124, Greece.
Rekka
Eleni A
EA
Siskou
Ioanna C
IC
Kourounakis
Panos N
PN
D000818:Animals; D000975:Antioxidants / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002784:Cholesterol / Q000097:blood; D000960:Hypolipidemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D066298:In Vitro Techniques; D015227:Lipid Peroxidation / Q000187:drug effects; D008077:Lipoproteins, LDL / Q000097:blood; D008862:Microsomes, Liver / Q000187:drug effects / Q000378:metabolism; D009025:Morpholines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D009566:Nitrates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D020030:Nitric Oxide Donors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship; D014280:Triglycerides / Q000097:blood
D000975:Antioxidants; D000960:Hypolipidemic Agents; D008077:Lipoproteins, LDL; D009025:Morpholines; D009566:Nitrates; D020030:Nitric Oxide Donors; D014280:Triglycerides; D002784:Cholesterol