Novel Sulfamide Analogs of Oleoylethanolamide Showing In Vivo Satiety Inducing Actions and PPARα Activation
摘要:
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 (PPAR alpha) 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 PPAR alpha.
The present invention is related to acyclic sulfamide derivatives, useful for the manufacture of a medicament for satiety induction and ingestion control, corporal fat modulation and lipidic metabolism regulation and for the manufacture of a medicament for the treatment or prevention of diabetes and cardiovascular diseases. The acyclic sulfamide derivatives are also useful for cosmetic use.
申请人:Fundacion Imabis. Inst. Meditteraneo para el
Avan e de la Biotecnologia y la Investigacion
Sanitaria
公开号:EP1984326B1
公开(公告)日:2017-05-03
US8188312B2
申请人:——
公开号:US8188312B2
公开(公告)日:2012-05-29
Novel Sulfamide Analogs of Oleoylethanolamide Showing In Vivo Satiety Inducing Actions and PPARα Activation
作者:Carolina Cano、Javier Pavón、Antonia Serrano、Pilar Goya、Juan Antonio Paez、Fernando Rodriguez de Fonseca、Manuel Macias-Gonzalez
DOI:10.1021/jm0601102
日期:2007.1.1
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 (PPAR alpha) 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 PPAR alpha.