Bacterial Topoisomerase Inhibitors:  Quinolone and Pyridone Antibacterial Agents

New rhenium complexes with ciprofloxacin as useful models for understanding the properties of [99mTc]-ciprofloxacin radiopharmaceutical

“…7,10,59 Different proposals have been made to understand the mechanism of Gyrase inhibition but the molecular details are unknown. 7,9,10,59 It should be mentioned that some authors support the idea that metal atoms are involved in the inhibitions mechanism of Gyrase by quinolones. For this reason, quinolones are also known as metallo-antibiotics, 60 and different studies on…”

“…Particularly, if we take into account that the atoms that probably interact with the metal (4-oxo carbonyl and carboxylate oxygen atoms) are the same that have been proposed to interact with DNA gyrase. 7,9 In contrast to this view, other authors have proposed that metal atoms can be involved in the interaction between ciprofloxacin and DNA-gyrase , 7,[18][19][20] which could A c c e p t e d m a n u s c r i p t 29 Zr, 29 Mo, 24 Ag, 30 Cd, 21,26 Pt, 31 U 32 and Eu 33 have been reported, and there is even a review of these metal complexes. 19 As mentioned above, the most common coordination mode of ciprofloxacin is through the oxygen atoms of the 4-oxo carbonyl and the carboxylate groups, forming a chelating ring of six atoms.…”

“…It is a synthetic antibiotic belonging to fluoroquinolone group with a broad-spectrum bacteria-localising capability. 7,8 Fluoroquinolones suppress the growth of bacteria by inhibiting the activity of DNA gyrase, an essential bacterial enzyme that relieves strain while double-stranded DNA is being unwound. 7,9,10 Technetium-99m labelled ciprofloxacin ( 99m Tc-ciprofloxacin or Infecton) was first introduced in the 1990s and has been extensively studied as an infection-specific radiopharmaceutical.…”

“…7,8 Fluoroquinolones suppress the growth of bacteria by inhibiting the activity of DNA gyrase, an essential bacterial enzyme that relieves strain while double-stranded DNA is being unwound. 7,9,10 Technetium-99m labelled ciprofloxacin ( 99m Tc-ciprofloxacin or Infecton) was first introduced in the 1990s and has been extensively studied as an infection-specific radiopharmaceutical. 5,[11][12][13][14][15][16] However, the global analysis of numerous published studies (including clinical trials) shows contradictory data about the specificity of 99m Tc-ciprofloxacin.…”

Coordenação de metais a antibióticos como uma estratégia de combate à resistência bacteriana

“…54,55 Alguns trabalhos apontam que o íon Mg(II) pode estar envolvido no modo de ação das fluorquinolonas, tendo importante papel na ligação destas substâncias ao complexo DNA-girase. [56][57][58] Porém, há outros que relatam que as fluorquinolonas perderiam atividade no organismo na presença do íon Mg(II), dentre outros. 59,60 Como já mencionado, a coordenação de íons metálicos a molécu-las que por si mesmas apresentam atividade antimicrobiana pode ser utilizada como uma importante estratégia para aumentar sua eficácia, inclusive em cepas resistentes.…”