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Triazolopyrimidine compounds containing first-row transition metals and their activity against the neglected infectious Chagas disease and leishmaniasis.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2014 Oct 06; Vol. 85, pp. 526-34. Date of Electronic Publication: 2014 Aug 10. - Publication Year :
- 2014
-
Abstract
- Leishmaniasis and Chagas disease remain a significant global problem. Current treatments have serious disadvantage due to cost, toxicity, long therapy duration and resistance. In the last years increasing interest has arisen in drug development to fight both diseases. Recently, metal-based drugs have revealed as promising drugs in a variety of therapeutic areas. Herein we describe six newly synthesized transition metal complexes with a bioactive molecule 5,7-dimethyl-1,2,4-triazolo[1,5-a]pyrimidine (dmtp). All of them have been characterized by X-ray, spectroscopic and thermal methods. In vitro and in vivo studies (murine model) on the antiproliferative activity of these complexes against Leishmania spp. (Leishmania infantum, Leishmania braziliensis) and Trypanosoma cruzi have been carried out. Our results reveal a strong potential of three of the assayed compounds as antiparasitic agents against the above-mentioned infectious diseases.<br /> (Copyright © 2014 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Animals
Chagas Disease drug therapy
Chlorocebus aethiops
Extracellular Space drug effects
Extracellular Space parasitology
Female
Inhibitory Concentration 50
Intracellular Space drug effects
Intracellular Space parasitology
Leishmania braziliensis drug effects
Leishmania infantum drug effects
Leishmaniasis drug therapy
Mice
Models, Molecular
Molecular Conformation
Organometallic Compounds therapeutic use
Organometallic Compounds toxicity
Trypanocidal Agents chemistry
Trypanocidal Agents pharmacology
Trypanocidal Agents therapeutic use
Trypanocidal Agents toxicity
Trypanosoma cruzi drug effects
Vero Cells
Chagas Disease parasitology
Leishmaniasis parasitology
Organometallic Compounds chemistry
Organometallic Compounds pharmacology
Transition Elements chemistry
Triazoles chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 85
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 25127147
- Full Text :
- https://doi.org/10.1016/j.ejmech.2014.08.026