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Title

Target-Accelerated Combinatorial Synthesis and Discovery of Highly Potent Antibiotics Effective Against Vancomycin-Resistant Bacteria

Authors
Nicolaou, K. C.
Hughes, Robert
Cho, Suk Young
Smethurst, Christian
Labischinski, Harald
Endermann, Rainer
Published in Angewandte Chemie: International Edition. 2000, vol. 39, no. 21, p. 3823-3828
Abstract 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.
Keywords AntibioticsCombinatorial chemistryDrug researchDrug-resistant bacteriaVancomycin
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NICOLAOU, K. C. et al. Target-Accelerated Combinatorial Synthesis and Discovery of Highly Potent Antibiotics Effective Against Vancomycin-Resistant Bacteria. In: Angewandte Chemie: International Edition, 2000, vol. 39, n° 21, p. 3823-3828. doi: 10.1002/1521-3773(20001103)39:21<3823::AID-ANIE3823>3.0.CO;2-3 https://archive-ouverte.unige.ch/unige:24512

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Deposited on : 2012-12-12

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