Similarity analysis, synthesis, and bioassay of antibacterial cyclic peptidomimetics

Faculty Pharmacy Year: 2012
Type of Publication: Article Pages: 1146-1160
Authors: DOI: 10.3762/bjoc.8.128
Journal: BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY BEILSTEIN-INSTITUT Volume: 8
Research Area: Chemistry ISSN ISI:000306830400002
Keywords : antibacterial, cluster analysis, N-acylbenzotriazoles, peptidomimetics, similarity    
Abstract:
The chemical similarity of antibacterial cyclic peptides and peptidomimetics was studied in order to identify new promising cyclic scaffolds. A large descriptor space coupled with cluster analysis was employed to digitize known antibacterial structures and to gauge the potential of new peptidomimetic macrocycles, which were conveniently synthesized by acylbenzotriazole methodology. Some of the synthesized compounds were tested against an array of microorganisms and showed antibacterial activity against Bordetella bronchistepica, Micrococcus luteus, and Salmonella typhimurium.
   
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