2. Academic Validation
  3. Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent

Fluorocyclines. 1. 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: a potent, broad spectrum antibacterial agent

  • J Med Chem. 2012 Jan 26;55(2):597-605. doi: 10.1021/jm201465w.
Xiao-Yi Xiao 1,  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
Affiliations

Affiliation

  • 1 Discovery Chemistry, Tetraphase Pharmaceuticals, 480 Arsenal Street, Watertown, Massachusetts 02472, United States. xyxiao@tphase.com
PMID: 22148514 DOI: 10.1021/jm201465w
Abstract

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).

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