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HPLC and 13C NMR for analysis of transamidation in a dynamic combinatorial chemistry system

Identyfikatory
Warianty tytułu
Języki publikacji
EN
Abstrakty
EN
The permanent demand for novel drugs by the pharmaceutical industry results in a variety of novel methods for drug discovery. Combinatorial methods are a novel direction of drug research based on synthesis of large number of compounds in the hope of finding interesting drug-like molecules. In dynamic combinatorial chemistry (DCC) an enzyme is used to control the synthetic path and increase the proportion of the drug-like molecules in the reaction mixture. Because the mixture formed by the reaction is complex, analytical procedures limit possible application of the method. In the work discussed in this publication HPLC was coupled with 13C NMR for analysis of a DCC system. Transamidation controlled by use of Candida rugosa lipase was compared with the reaction without the enzyme. This enabled us to show that the enzyme-promoted reaction favoured the amine with the lowest nucleophilicity.
Słowa kluczowe
EN
Rocznik
Tom
Strony
314--319
Opis fizyczny
Bibliogr. 11 poz., rys.
Twórcy
autor
autor
autor
autor
autor
  • Institute of Chemistry, University of Silesia, Szkolna 9, 40-006 Katowice, Poland
Bibliografia
  • [1] T. Langer and R.D. Hoffmann, Curr. Pharm. Des., 7, 509 (2001)
  • [2] H. Kubinyi, Curr. Opin. Drug Discov. Dev., 1, 16 (1998)
  • [3] H. Kubinyi, Nat. Rev. Drug Discov., 2, 665 (2003)
  • [4] I. Huc and R. Nguyen, Combin. Chem. High Throughput Screen., 4, 53 (2001)
  • [5] J.M. Lehn, Chem. Eur. J., 5, 2455 (1999)
  • [6] S. Otto, R.L. Furlan, and J.K. Sanders, Drug Discov. Today, 7, 117 (2002)
  • [7] H. Niedbała, R. Musioł, A. Pałka, B. Podeszwa, A. Mencel, D. Tabak, J. Polański, and J. Finster, Pol. Pat. Appl. P3741130 (2005)
  • [8] S.E. Eldred, D.A. Stone, S.H. Gellmann, and S.S. Stahl, J. Am. Chem. Soc., 25, 3422 (2003)
  • [9] B. Fleckenstein, O. Molberg, S.W. Qiao, D.G. Schmid, F. von der Mülbe, K. Elgstoen, G. Jung, and L.M. Sollid, J. Biol. Chem., 277, 34109 (2002)
  • [10] J.S. Fruton, R.B. Johnston, and M. Fried, J. Biol. Chem., 190, 39 (1951)
  • [11] M.V. Sergeeva, V.V. Mozhaev, J.O. Rich, and Y.L. Khmielnitsky, Biotech. Lett., 22, 1419 (2000)
Typ dokumentu
Bibliografia
Identyfikator YADDA
bwmeta1.element.baztech-article-BAT8-0006-0058
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