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

Roger B. Clark | Zendy; Minsheng He | Zendy; Corey Fyfe | Zendy; Denene Lofland | Zendy; William J. O’Brien | Zendy; Louis Plamondon | Zendy; Joyce A. Sutcliffe | Zendy; Xiao-Yi Xiao | Zendy

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

Author(s) -

Roger B. Clark,

Minsheng He,

Corey Fyfe,

Denene Lofland,

William J. O’Brien,

Louis Plamondon,

Joyce A. Sutcliffe,

Xiao-Yi Xiao

Publication year - 2011

Publication title -

journal of medicinal chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.01

H-Index - 261

eISSN - 1520-4804

pISSN - 0022-2623

DOI - 10.1021/jm1015389

Subject(s) - tetracycline , chemistry , efflux , antibacterial activity , in vivo , gram , antibacterial agent , microbiology and biotechnology , antibiotics , combinatorial chemistry , bacteria , biochemistry , biology , genetics

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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