Thiourea-based gemfibrozil analogues as HDL-elevating agents.
A series of gemfibrozil analogues with a thiourea moiety embedded in the side chain was prepared and evaluated as HDL-elevating agents. Derivatives 8b, 9b, 9c, and 9d were found to be approximately as effective as gemfibrozil (1) for HDL cholesterol elevation.
Coppola
Gary M
GM
Department of Metabolic and Cardiovascular Diseases, Novartis Institute for Biomedical Research, Summit, NJ 07901, USA. gary.coppola@pharma.novartis.com
Damon
Robert E
RE
Eskesen
J Bruce
JB
France
Dennis S
DS
Paterniti
James R
JR
D000284:Administration, Oral; D000818:Animals; D016632:Apolipoprotein A-I / Q000097:blood / Q000187:drug effects; D015248:Gemfibrozil / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D000960:Hypolipidemic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D008075:Lipoproteins, HDL / Q000097:blood / Q000187:drug effects*; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship; D013890:Thiourea / Q000138:chemical synthesis / Q000494:pharmacology
D016632:Apolipoprotein A-I; D000960:Hypolipidemic Agents; D008075:Lipoproteins, HDL; D013890:Thiourea; D015248:Gemfibrozil