1-Hydroxyalkyl-3-phenylthioureas as novel HDL-elevating agents.
A series of 1-hydroxyalkyl-3-phenylthiourea analogs were prepared and evaluated as HDL-and Apo A-I-elevating agents. Derivatives 5h, 7j, 7n, and 7o were found to be as effective or superior to gemfibrozil.
Coppola
Gary M
GM
Department of Diabetes and Metabolism, Novartis Institutes for Biomedical Research, 100 Technology Square, Cambridge, MA 02139, USA. gary.oppola@pharma.novartis.com
Damon
Robert E
RE
Eskesen
J Bruce
JB
France
Dennis S
DS
Paterniti
James R
JR
D000818:Animals; D016632:Apolipoprotein A-I / Q000097:blood / Q000187:drug effects; D002784:Cholesterol / Q000008:administration & dosage / Q000097:blood; D006801:Humans; D008055:Lipids / Q000097:blood; D008075:Lipoproteins, HDL / Q000097:blood / Q000187:drug effects*; D008297:Male; D010670:Phenylthiourea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship; D015430:Weight Gain / Q000187:drug effects
D016632:Apolipoprotein A-I; D008055:Lipids; D008075:Lipoproteins, HDL; D010670:Phenylthiourea; D002784:Cholesterol