In vitro advanced antimycobacterial screening of cobalt(II) and copper(II) complexes of fluorinated isonicotinoylhydrazones.
The in vitro antimycobacterial activity of cobalt(II) and copper(II) complexes of some fluorinated isonicotinoylhydrazones was evaluated in a TB-infected macrophage model; all metalcomplexes exhibited excellent activity against Mycobacterium tuberculosis Erdman growing within macrophages, at concentrations much lower than in culture media. Moreover complexes 1b and 2a displayed EC(99) values lower than that of the parent-drug, isoniazid. In addition, all tested metalchelates significantly inhibited the growth of single-drug-resistant M. tuberculosis strains; complexes 1a and 2a also possessed moderate activity against Mycobacterium avium complex.
Maccari
Rosanna
R
Dipartimento Farmaco-chimico, Facoltà di Farmacia, Università di Messina, Viale SS. Annunziata, 98168 Messina, Italy. rmaccari@pharm.unime.it
Ottanà
Rosaria
R
Bottari
Bruno
B
Rotondo
Enrico
E
Vigorita
Maria Gabriella
MG
D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D003035:Cobalt / Q000737:chemistry / Q000494:pharmacology*; D003300:Copper / Q000737:chemistry / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical / Q000379:methods; D005461:Fluorine / Q000737:chemistry / Q000494:pharmacology; D006835:Hydrazones / Q000737:chemistry / Q000494:pharmacology; D007538:Isoniazid / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D008826:Microbial Sensitivity Tests / Q000706:statistics & numerical data; D009169:Mycobacterium tuberculosis / Q000187:drug effects* / Q000502:physiology
D000900:Anti-Bacterial Agents; D006835:Hydrazones; D005461:Fluorine; D003035:Cobalt; D003300:Copper; D007538:Isoniazid