title: Microwave-assisted synthesis of a novel class of imidazolylthiazolidin-4-ones and evaluation of its biological activities.
abstract: The synthesis and biological activity of a hitherto unknown class of compounds, the imidazolylthiazolidin-4-ones, are described. A two-step procedure has been elaborated starting from our previously described 2-aminoimidazoles. The application of microwave irradiation has been proven to be beneficial for the condensation of the imine with mercaptoacetic acid leading to the formation of imidazolylthiazolidin-4-ones. None of the compounds showed antiviral activity at subtoxic concentrations. Several compounds displayed a moderate cytostatic activity. These data form the basis for further improvement of the potential antiproliferative activity of this class of compounds.
authors.affiliation: Laboratory for Organic and Microwave-Assisted Chemistry (LOMAC), Department of Chemistry, Katholieke Universiteit Leuven, Celestijnenlaan 200F, 3001, Leuven, Belgium.
authors.forename: Sachin G
authors.initials: SG
authors.lastname: Modha
authors.forename: Vaibhav P
authors.initials: VP
authors.lastname: Mehta
authors.forename: Denis
authors.initials: D
authors.lastname: Ermolat'ev
authors.forename: Jan
authors.initials: J
authors.lastname: Balzarini
authors.forename: Kristof
authors.initials: K
authors.lastname: Van Hecke
authors.forename: Luc
authors.initials: L
authors.lastname: Van Meervelt
authors.forename: Erik
authors.initials: E
authors.lastname: Van der Eycken
mesh_terms: D000818:Animals; D002384:Catalysis / Q000528:radiation effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002625:Chemistry, Organic / Q000379:methods; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D006801:Humans; D007093:Imidazoles / Q000737:chemistry; D051379:Mice; D008826:Microbial Sensitivity Tests; D008872:Microwaves; D008954:Models, Biological; D008958:Models, Molecular; D008968:Molecular Conformation; D045162:Thiazolidinediones / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D007093:Imidazoles; D045162:Thiazolidinediones; C014973:2-aminoimidazole