title: Synthesis and biological activity of [[(heterocycloamino)alkoxy] benzyl]-2,4-thiazolidinediones as PPARgamma agonists.
abstract: Benzothiazole derivatives of thiazolidinediones (TZD) were synthesized using a modified Mitsunobu reaction of 2-(benzothiazol-2-ylmethylamino)ethanol (2) with 5-(4-hydroxybenzyl)-3-triphenylmethylthiazolidine-2,4-dione and assayed for activity on peroxisome proliferator-activated receptor (PPAR) subtypes and inhibitory activity of NO production in lipopolysaccharide-activated macrophages. Most of the tested compounds were identified as potent PPARgamma agonists, indicating their potential as drug candidates for diabetes.
authors.affiliation: College of Pharmacy, Sookmyung Women's University, Seoul 140-742, Korea. rjeon@sookmyung.ac.kr
authors.forename: Raok
authors.initials: R
authors.lastname: Jeon
authors.forename: Yoon-Jung
authors.initials: YJ
authors.lastname: Kim
authors.forename: Yejin
authors.initials: Y
authors.lastname: Cheon
authors.forename: Jae-Ha
authors.initials: JH
authors.lastname: Ryu
mesh_terms: D000818:Animals; D052160:Benzothiazoles / Q000138:chemical synthesis / Q000494:pharmacology; D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D007004:Hypoglycemic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D008070:Lipopolysaccharides; D008264:Macrophages / Q000187:drug effects* / Q000378:metabolism; D051379:Mice; D015394:Molecular Structure; D009573:Nitrites / Q000378:metabolism; D047495:PPAR gamma / Q000819:agonists* / Q000235:genetics; D013329:Structure-Activity Relationship; D045162:Thiazolidinediones / Q000138:chemical synthesis / Q000494:pharmacology*; D014162:Transfection
chemical_list: D052160:Benzothiazoles; D007004:Hypoglycemic Agents; D008070:Lipopolysaccharides; D009573:Nitrites; D047495:PPAR gamma; D045162:Thiazolidinediones