title: Solution-phase parallel synthesis of a 1140-member ureidothiophene carboxylic acid library.
abstract: A 1140-library of thiophene ureidoacids was synthesized by the reaction of a set of 60 primary or secondary amines with a number of 19 thieno[3,2-d]- or thieno[2,3-d][1,3]oxazine-2,4-diones. All compounds were obtained by a simple solution-phase combinatorial strategy on a 200-400-mg scale with over 70% yields and purities over 80%. Sixty library members chosen at random were successfully characterized by standard 1H NMR, HPLC/MS, and IR studies. Analgesic, antalgic, and antiinflammatory potential were investigated. The 1140-member ureidothiophene carboxylic acid library will be used in high-throughput screening assays.
authors.affiliation: Centre d'Etudes et de Recherche sur le Médicament de Normandie, 5 rue Vaubénard, 14032 Caen Cedex, France.
authors.forename: François-Xavier
authors.initials: FX
authors.lastname: Le Foulon
authors.forename: Emmanuelle
authors.initials: E
authors.lastname: Braud
authors.forename: Frédéric
authors.initials: F
authors.lastname: Fabis
authors.forename: Jean-Charles
authors.initials: JC
authors.lastname: Lancelot
authors.forename: Sylvain
authors.initials: S
authors.lastname: Rault
mesh_terms: D002264:Carboxylic Acids / Q000138:chemical synthesis* / Q000737:chemistry; D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D015195:Drug Design; D015394:Molecular Structure; D013876:Thiophenes / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D002264:Carboxylic Acids; D013876:Thiophenes