Design, Synthesis, and Biological Evaluation of Hexacyclic Tetracyclines as Potent, Broad Spectrum Antibacterial Agents

Journal of Medicinal Chemistry
2015.0

Abstract

A series of novel hexacyclic tetracycline analogues ("hexacyclines") was designed, synthesized, and evaluated for antibacterial activity against a wide range of clinically important bacteria isolates, including multidrug-resistant, Gram-negative pathogens. Valuable structure-activity relationships were identified, and several hexacyclines displayed potent, broad spectrum antibacterial activity, including promising anti-Pseudomonas aeruginosa activity in vitro and in vivo.

Knowledge Graph

Similar Paper

Design, Synthesis, and Biological Evaluation of Hexacyclic Tetracyclines as Potent, Broad Spectrum Antibacterial Agents
Journal of Medicinal Chemistry 2015.0
Heterocyclyl Tetracyclines. 1. 7-Trifluoromethyl-8-Pyrrolidinyltetracyclines: Potent, Broad Spectrum Antibacterial Agents with Enhanced Activity against Pseudomonas aeruginosa
Journal of Medicinal Chemistry 2017.0
Synthesis and Antibacterial Activity of Pentacyclines: A Novel Class of Tetracycline Analogs
Journal of Medicinal Chemistry 2011.0
Glycylcyclines. 1. A new generation of potent antibacterial agents through modification of 9-aminotetracyclines
Journal of Medicinal Chemistry 1994.0
8-Azatetracyclines: Synthesis and Evaluation of a Novel Class of Tetracycline Antibacterial Agents
Journal of Medicinal Chemistry 2011.0
Fluorocyclines. 1. 7-Fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: A Potent, Broad Spectrum Antibacterial Agent
Journal of Medicinal Chemistry 2012.0
Synthesis, antimicrobial activity and structure–activity relationship study of N,N-dibenzyl-cyclohexane-1,2-diamine derivatives
European Journal of Medicinal Chemistry 2011.0
Dactylocyclines, novel tetracycline derivatives produced by a Dactylosporangium sp. I. Taxonomy, production, isolation and biological activity.
The Journal of Antibiotics 1992.0
Fluorocyclines. 2. Optimization of the C-9 Side-Chain for Antibacterial Activity and Oral Efficacy
Journal of Medicinal Chemistry 2012.0
Synthesis and Characterization of Tetrahydropyran-Based Bacterial Topoisomerase Inhibitors with Antibacterial Activity against Gram-Negative Bacteria
Journal of Medicinal Chemistry 2017.0