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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.

SUBMITTER: Clark RB

PROVIDER: S-EPMC3103189 | biostudies-literature | 2011 Mar

REPOSITORIES: biostudies-literature

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

Clark Roger B RB He Minsheng M Fyfe Corey C Lofland Denene D O'Brien William J WJ Plamondon Louis L Sutcliffe Joyce A JA Xiao Xiao-Yi XY

Journal of medicinal chemistry 20110208 5

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. ...[more]

PMID: 21302930

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