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8-Azatetracyclines: synthesis and evaluation of a novel class of tetracycline antibacterial agents.

Abstract：

: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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Clark RB,He M,Fyfe C,Lofland D,O'Brien WJ,Plamondon L,Sutcliffe JA,Xiao XY

doi

10.1021/jm1015389

subject

Has Abstract

pub_date

2011-03-10 00:00:00

pages

1511-28

issue

5

eissn

0022-2623

issn

1520-4804

journal_volume

54

pub_type

杂志文章

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