Effects of 2-(substituted-sulfanyl)-3,5-dihydro-imidazole-4-one and 2-(substituted-sulfanyl)-1H-imidazole-4,5-dione derivatives on serum HDL-cholesterol.
A series of 2-substituted sulfanyl-3,5-dihydro-imidazole-4-ones and 2-substituted sulfanyl-1H-imidazole-4,5-diones was prepared and shown to increase high density lipoprotein cholesterol over other lipid fractions. Compound 1f showed efficacy in additional animal models. The major metabolite of 1f was isolated and its synthesis is reported. The effects of the metabolite on the lipid profile in rats were investigated.
Elokdah
H
H
Medicinal Chemistry, Chemical Sciences, Wyeth-Ayerst Research, Princeton, NJ 08543, USA. elokdah@war.wyeth.com
Sulkowski
T
T
Cochran
D
D
McKean
M L
ML
Quinet
E
E
D000818:Animals; D000924:Anticholesteremic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D002784:Cholesterol / Q000008:administration & dosage; D008076:Cholesterol, HDL / Q000097:blood* / Q000378:metabolism; D008078:Cholesterol, LDL / Q000097:blood; D015243:Cholesterol, VLDL / Q000097:blood; D006224:Cricetinae; D006801:Humans; D007093:Imidazoles / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008074:Lipoproteins / Q000097:blood; D008297:Male; D008862:Microsomes, Liver / Q000378:metabolism; D015394:Molecular Structure; D051381:Rats
D000924:Anticholesteremic Agents; D008076:Cholesterol, HDL; D008078:Cholesterol, LDL; D015243:Cholesterol, VLDL; D007093:Imidazoles; D008074:Lipoproteins; D002784:Cholesterol