20. Target-Accelerated Combinatorial Synthesis and Discovery of Highly Potent Antibiotics Effective Against Vancomycin-Resistant Bacteria
    K. C. Nicolaou, R. Hughes, S. Y. Cho, N. Winssinger, C. Smethurst, H. Labischinski, R. Endermann
    Angew. Chem. Int. Ed. 2000, 39, 3823-3828

Biological activity can be predicted at a prescreening stage by using a target-accelerated combinatorial synthesis. The rate of dimerization of vancomycin analogues (see picture, X=CH=CH₂, SAc) in the presence of vancomycin's targets Ac-d-Ala-d-Ala and Ac₂-l-Lys-d-Ala-d-Ala correlated well with the observed biological activity. From this study three highly potent antibacterial agents effective against both vancomycin-susceptible and vancomycin-resistant bacteria strains were identified.

DOI : 10.1002/1521-3773(20001103)39:21<3823::AID-ANIE3823>3.0.CO;2-3 

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