8-Azatetracyclines: Synthesis and Evaluation of a Novel Class of Tetracycline Antibacterial Agents

[Image: see text] A novel series of fully synthetic 8-azatetracyclines was prepared and evaluated for antibacterial activity. Compounds were identified that overcome both efflux (tet(K)) and ribosomal protection (tet(M)) tetracycline resistance mechanisms and are active against Gram-positive and Gra...

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Detalles Bibliográficos
Autores principales: Clark, Roger B., He, Minsheng, Fyfe, Corey, Lofland, Denene, O’Brien, William J., Plamondon, Louis, Sutcliffe, Joyce A., Xiao, Xiao-Yi
Formato: Texto
Lenguaje:English
Publicado: American Chemical Society 2011
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3103189/
https://www.ncbi.nlm.nih.gov/pubmed/21302930
http://dx.doi.org/10.1021/jm1015389
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author Clark, Roger B.
He, Minsheng
Fyfe, Corey
Lofland, Denene
O’Brien, William J.
Plamondon, Louis
Sutcliffe, Joyce A.
Xiao, Xiao-Yi
author_facet Clark, Roger B.
He, Minsheng
Fyfe, Corey
Lofland, Denene
O’Brien, William J.
Plamondon, Louis
Sutcliffe, Joyce A.
Xiao, Xiao-Yi
author_sort Clark, Roger B.
collection PubMed
description [Image: see text] A novel series of fully synthetic 8-azatetracyclines was prepared and evaluated for antibacterial activity. Compounds were identified that overcome both efflux (tet(K)) and ribosomal protection (tet(M)) tetracycline resistance mechanisms and are active against Gram-positive and Gram-negative organisms. Two compounds were identified that exhibit comparable efficacy to marketed tetracyclines in in vivo models of bacterial infection.
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spelling pubmed-31031892011-05-27 8-Azatetracyclines: Synthesis and Evaluation of a Novel Class of Tetracycline Antibacterial Agents Clark, Roger B. He, Minsheng Fyfe, Corey Lofland, Denene O’Brien, William J. Plamondon, Louis Sutcliffe, Joyce A. Xiao, Xiao-Yi J Med Chem [Image: see text] A novel series of fully synthetic 8-azatetracyclines was prepared and evaluated for antibacterial activity. Compounds were identified that overcome both efflux (tet(K)) and ribosomal protection (tet(M)) tetracycline resistance mechanisms and are active against Gram-positive and Gram-negative organisms. Two compounds were identified that exhibit comparable efficacy to marketed tetracyclines in in vivo models of bacterial infection. American Chemical Society 2011-02-08 2011-03-10 /pmc/articles/PMC3103189/ /pubmed/21302930 http://dx.doi.org/10.1021/jm1015389 Text en Copyright © 2011 American Chemical Society http://pubs.acs.org This is an open-access article distributed under the ACS AuthorChoice Terms & Conditions. Any use of this article, must conform to the terms of that license which are available at http://pubs.acs.org.
spellingShingle Clark, Roger B.
He, Minsheng
Fyfe, Corey
Lofland, Denene
O’Brien, William J.
Plamondon, Louis
Sutcliffe, Joyce A.
Xiao, Xiao-Yi
8-Azatetracyclines: Synthesis and Evaluation of a Novel Class of Tetracycline Antibacterial Agents
title 8-Azatetracyclines: Synthesis and Evaluation of a Novel Class of Tetracycline Antibacterial Agents
title_full 8-Azatetracyclines: Synthesis and Evaluation of a Novel Class of Tetracycline Antibacterial Agents
title_fullStr 8-Azatetracyclines: Synthesis and Evaluation of a Novel Class of Tetracycline Antibacterial Agents
title_full_unstemmed 8-Azatetracyclines: Synthesis and Evaluation of a Novel Class of Tetracycline Antibacterial Agents
title_short 8-Azatetracyclines: Synthesis and Evaluation of a Novel Class of Tetracycline Antibacterial Agents
title_sort 8-azatetracyclines: synthesis and evaluation of a novel class of tetracycline antibacterial agents
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3103189/
https://www.ncbi.nlm.nih.gov/pubmed/21302930
http://dx.doi.org/10.1021/jm1015389
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