Triazolopyrimidine compounds containing first-row transition metals and their activity against the neglected infectious Chagas disease and leishmaniasis.


Caballero, AB; Rodríguez-Diéguez, A; Quirós, M; Salas, JM; Huertas, Ó, ; Ramírez-Macías, I; Olmo, F; Marín, C; Chaves-Lemaur, G; Gutierrez-Sánchez, R; Sánchez-Moreno, M; (2014) Triazolopyrimidine compounds containing first-row transition metals and their activity against the neglected infectious Chagas disease and leishmaniasis. European journal of medicinal chemistry, 85. pp. 526-34. ISSN 0223-5234 DOI: https://doi.org/10.1016/j.ejmech.2014.08.026

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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.

Item Type: Article
Faculty and Department: Faculty of Infectious and Tropical Diseases > Dept of Pathogen Molecular Biology
Research Centre: Neglected Tropical Diseases Network
PubMed ID: 25127147
Web of Science ID: 342859700045
URI: http://researchonline.lshtm.ac.uk/id/eprint/2909340

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