Target-Accelerated Combinatorial Synthesis and Discovery of Highly Potent Antibiotics Effective Against Vancomycin-Resistant Bacteria
Year: 2000
Type: article
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.
Authors: K. C. Nicolaou, Robert Hughes, Suk Young Cho, Nicolas Winssinger, Christian Smethurst, Harald Labischinski, Rainer Endermann
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: green
OpenAlex ID: W2140172630