Novel sulfamide analogs of oleoylethanolamide showing in vivo satiety inducing actions and PPARalpha activation.
Long chain saturated and unsaturated alkyl sulfamide and propyl sulfamide derivatives, analogs of oleoylethanolamide, have been synthesized and evaluated in vivo and in vitro as peroxisome proliferator activated receptor alpha (PPARalpha) activators. Additionally, the anorexic effects of the new compounds have been studied in vivo in food-deprived rats. Among the active compounds N-octadecyl-N'-propylsulfamide (7) has been identified as a potent hypolipidemic compound, a potent feeding suppressant, and a concentration-dependent activator of PPARalpha.
Cano
Carolina
C
Instituto de Química Médica, CSIC, Juan de la Cierva 3, 28006, Madrid, Spain.
Pavón
Javier
J
Serrano
Antonia
A
Goya
Pilar
P
Paez
Juan Antonio
JA
de Fonseca
Fernando Rodriguez
FR
Macias-Gonzalez
Manuel
M
D000818:Animals; D001067:Appetite Depressants / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D003065:Coenzyme A / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004435:Eating / Q000187:drug effects; D063388:Endocannabinoids; D005508:Food Deprivation; D017930:Genes, Reporter; D006801:Humans; D000960:Hypolipidemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008156:Luciferases / Q000096:biosynthesis / Q000235:genetics; D009829:Oleic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D047493:PPAR alpha / Q000819:agonists* / Q000235:genetics / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D011924:Rats, Zucker; D012527:Satiation / Q000187:drug effects*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015533:Transcriptional Activation; D014162:Transfection
D001067:Appetite Depressants; D063388:Endocannabinoids; D000960:Hypolipidemic Agents; C517808:N-octadecyl-N'-propylsulfamide; D009829:Oleic Acids; D047493:PPAR alpha; D013449:Sulfonamides; C488250:oleoylethanolamide; D008156:Luciferases; D003065:Coenzyme A