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Ruthenium(II) phosphine/diimine/picolinate complexes: inorganic compounds as agents against tuberculosis.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2011 Oct; Vol. 46 (10), pp. 5099-107. Date of Electronic Publication: 2011 Aug 23. - Publication Year :
- 2011
-
Abstract
- This paper describes the synthesis and characterization of four new ruthenium complexes containing 1,4 bis(diphenylphosphino)butane (dppb), 2-pyridinecarboxylic acid anion (pic) and the diimines [(2,2'-bipyridine (bipy), 4,4'-dimethyl-2,2'-bipyridine (Me-bipy), 4,4'-dichloro-2,2'-bipyridine (Cl-bipy) and 1,10-phenanthroline (phen) as ligands, with formulae [Ru(pic)(dppb)(bipy)]PF(6) (SCAR01), [Ru(pic)(dppb)(Me-bipy)]PF(6) (SCAR02), [Ru(pic)(dppb)(Cl-bipy)]PF(6) (SCAR03) and [Ru(pic)(dppb)(phen)]PF(6) (SCAR04). Additionally, the in vitro anti-Mycobacterium tuberculosis (MTB) activity, cytotoxicity and activity against in vitro infection of these complexes and two more complexes, cis-[Ru(pic)(dppe)(2)]PF(6) (SCAR05) and cis-[RuCl(2)(dppb)(bipy)] (SCAR06), and their free ligands are described and discussed. All compounds showed excellent MIC against MTB, low cytotoxicity and a selectivity index higher than 10. Also, all compounds showed significant intracellular inhibition and the compound SCAR05 showed a better activity than rifampin and SQ109. This is the first report of activity against in vitro infection of ruthenium compounds.<br /> (Copyright © 2011 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Animals
Antitubercular Agents chemistry
Cell Line
Crystallography, X-Ray
Humans
Imines chemistry
Mice
Models, Molecular
Organometallic Compounds pharmacology
Phosphines chemistry
Picolinic Acids chemistry
Ruthenium chemistry
Tuberculosis drug therapy
Antitubercular Agents pharmacology
Imines pharmacology
Mycobacterium tuberculosis drug effects
Phosphines pharmacology
Picolinic Acids pharmacology
Ruthenium pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 46
- Issue :
- 10
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 21875763
- Full Text :
- https://doi.org/10.1016/j.ejmech.2011.08.023