Synthesis and In Vitro Antimycobacterial and Antibacterial Activity of 8-OMe Ciprofloxacin-Hydrozone/Azole Hybrids

Molecules. 2017 Jul 13;22(7):1171. doi: 10.3390/molecules22071171.

Abstract

A series of novel 8-OMe ciprofloxacin (CPFX)-hydrazone/azole hybrids were designed, synthesized, and evaluated for their in vitro biological activities. Our results reveal that all of the hydrozone-containing hybrids (except for 7) show potency against Mycobacterium tuberculosis (MTB) H37Rv (minimum inhibitory concentration (MIC): <0.5 μM), which is better than the parent drug CPFX, and comparable to moxifloxacin and isoniazid, some of the tested Gram-positive strains (MIC: 0.06-4 μg/mL), and most Gram-negative strains (MIC: ≤0.03-4 μg/mL).

Keywords: 8-OMe ciprofloxacin; antibacterial; antimycobacterial; hybrids; synthesis.

MeSH terms

  • Animals
  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Antitubercular Agents / chemical synthesis
  • Antitubercular Agents / chemistry
  • Antitubercular Agents / pharmacology
  • Azoles / chemical synthesis
  • Azoles / chemistry
  • Azoles / pharmacology
  • Ciprofloxacin / analogs & derivatives
  • Ciprofloxacin / chemical synthesis
  • Ciprofloxacin / chemistry*
  • Ciprofloxacin / pharmacology
  • Humans
  • Hydrozoa / chemistry
  • Microbial Sensitivity Tests
  • Mycobacterium tuberculosis / drug effects*
  • Mycobacterium tuberculosis / pathogenicity
  • Tuberculosis / drug therapy*
  • Tuberculosis / microbiology

Substances

  • Anti-Bacterial Agents
  • Antitubercular Agents
  • Azoles
  • Ciprofloxacin