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      An Expedient and Facile One-Step Synthesis of a Biguanide Library by Microwave Irradiation Coupled with Simple Product Filtration. Inhibitors of Dihydrofolate Reductase

      , , , ,

      Journal of Combinatorial Chemistry

      American Chemical Society (ACS)

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          Abstract

          It has been demonstrated previously by us that guanide-containing compounds (1 and 2) can inhibit significantly dihydrofolate reductase (DHFR). In this report, we have produced an array of alkyl- and aryl-based biguanide compounds using microwave irradiation. Further, we have demonstrated the use of TMSCl for the first time as an excellent and practical catalyst for the formation of alkyl and aryl biguanides. Using these methods, we prepared a 60-compound collection, of which one compound (21g) showed approximately one-half of the inhibitory activity of the parent compound 2.

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          Author and article information

          Journal
          Journal of Combinatorial Chemistry
          J. Comb. Chem.
          American Chemical Society (ACS)
          1520-4766
          1520-4774
          September 2004
          September 2004
          : 6
          : 5
          : 776-782
          Article
          10.1021/cc049953+
          15360213
          © 2004
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