Design, synthesis and evaluation of D,D-peptidase and beta-lactamase inhibitors: azapeptides, oxapeptides and related heterocycles.

Marchand-Brynaert, Jacqueline;Mougenot, P;Combret, Y;Belotti, D;Ghosez, Léon;et.al.
(1995) Il Farmaco — Vol. 50, n° 6, p. 455-469 (1995)

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  • Marchand-Brynaert, JacquelineUCLouvain
    Author
  • Mougenot, P
    Author
  • Combret, Y
    Author
  • Belotti, D
    Author
  • Ghosez, LéonUCLouvain
    Author
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Abstract
Reactive molecules susceptible to form stable acyl enzyme intermediates with D,D-peptidases and beta-lactamases were designed as potential irreversible inhibitors of Penicillin Sensitive Enzymes (PSEs). The structures examined were a series of azapeptides and oxapeptides, both analogs of the D-Ala-D-Ala substrate, and some heterocycles, such as imidazolidinones and oxazolidinones, both analogs of the beta-lactam antibiotics. The various strategies investigated for their synthesis are described and discussed. Some biological results are reported.
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Marchand-Brynaert, J., Mougenot, P., Combret, Y., Belotti, D., Guillot, N., & Ghosez, L. (1995). Design, synthesis and evaluation of D,D-peptidase and beta-lactamase inhibitors: azapeptides, oxapeptides and related heterocycles. Il Farmaco, 50(6), 455-469. https://hdl.handle.net/2078.5/134805 (Original work published 1995)