Activity of new N-acylated ciprofloxacin derivatives against faculative intracellular bacteria

US8143398B1 · kind B1 · utility

Assignee

• University of South Florida · US

Inventors

• Edward Turos · Tampa, US
• Burt Anderson · Tucker, US
• Ryan Scott Cormier · Morton, US
• John Carl Thomas · Sunnyvale, US
• Rebecca J. Kapolka · Pinellas Park, US
• Glenn Roma · Tampa, US

Key dates

• Filing date: Feb 22, 2011
• Grant date: Mar 27, 2012
• Expiry date: Feb 22, 2031

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D241/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Bartonella species are facultative intracellular pathogens responsible for a range of diseases in animals and in humans. A selection of N-acyl ciprofloxacin analogues, chemically synthesized from ciprofloxacin, have been tested in vitro for activity against Bartonella species as models for therapeutic development. Nine Bartonella strains, including five of B. henselae, two of B. quintana, and one each of B. elizabethae and B. vinsonii, have been tested for susceptibility to different N-acyl ciprofloxacin derivatives. Several techniques have been used to test the in vitro antibacterial activity of the derivatives. Seven of them, labeled RC4-125, RC4-143, RC4-147, RC5-28, RC5-29, RC5-32 and RC5-69 showed significant intracellular anti-Bartonella activity. These synthetically derived N-acyl ciprofloxacin derivatives may be useful in the therapeutic treatment of infections caused by Bartonella.