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  • Title: Solution-phase parallel synthesis of a 1140-member ureidothiophene carboxylic acid library.
    Author: Le Foulon FX, Braud E, Fabis F, Lancelot JC, Rault S.
    Journal: J Comb Chem; 2005; 7(2):253-7. PubMed ID: 15762753.
    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.
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