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Fluorocyclines. 1. 7-Fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: A Potent, Broad Spectrum Antibacterial Agent

2011; American Chemical Society; Volume: 55; Issue: 2 Linguagem: Inglês

10.1021/jm201465w

1520-4804

Xiao-Yi Xiao, Diana K. Hunt, Jingye Zhou, Roger B. Clark, Nick Dunwoody, Corey Fyfe, Trudy H. Grossman, William J. O’Brien, Louis Plamondon, Magnus Rönn, Cuixiang Sun, Wu‐Yan Zhang, Joyce A. Sutcliffe,

Cancer therapeutics and mechanisms

This and the accompanying report (DOI: 10.1021/jm201467r ) describe the design, synthesis, and evaluation of a new generation of tetracycline antibacterial agents, 7-fluoro-9-substituted-6-demethyl-6-deoxytetracyclines ("fluorocyclines"), accessible through a recently developed total synthesis approach. These fluorocyclines possess potent antibacterial activities against multidrug resistant (MDR) Gram-positive and Gram-negative pathogens. One of the fluorocyclines, 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline (17j, also known as TP-434, 50th Interscience Conference on Antimicrobial Agents and Chemotherapy Conference , Boston, MA , September 12-15, 2010 , poster F1 - 2157 ), is currently undergoing phase 2 clinical trials in patients with complicated intra-abdominal infections (cIAI).