title: Triazolopyrimidine compounds containing first-row transition metals and their activity against the neglected infectious Chagas disease and leishmaniasis.
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.
authors.affiliation: Departamento de Química Inorgánica, Universidad de Granada, Severo Ochoa s/n, E-18071 Granada, Spain.
authors.forename: Ana B
authors.initials: AB
authors.lastname: Caballero
authors.affiliation: Departamento de Química Inorgánica, Universidad de Granada, Severo Ochoa s/n, E-18071 Granada, Spain.
authors.forename: Antonio
authors.initials: A
authors.lastname: Rodríguez-Diéguez
authors.affiliation: Departamento de Química Inorgánica, Universidad de Granada, Severo Ochoa s/n, E-18071 Granada, Spain.
authors.forename: Miguel
authors.initials: M
authors.lastname: Quirós
authors.affiliation: Departamento de Química Inorgánica, Universidad de Granada, Severo Ochoa s/n, E-18071 Granada, Spain. Electronic address: jsalas@ugr.es.
authors.forename: Juan M
authors.initials: JM
authors.lastname: Salas
authors.affiliation: Departamento de Parasitología, Universidad de Granada, Severo Ochoa s/n, E-18071 Granada, Spain.
authors.forename: Óscar
authors.initials: Ó
authors.lastname: Huertas
authors.affiliation: Departamento de Parasitología, Universidad de Granada, Severo Ochoa s/n, E-18071 Granada, Spain.
authors.forename: Inmaculada
authors.initials: I
authors.lastname: Ramírez-Macías
authors.affiliation: Departamento de Parasitología, Universidad de Granada, Severo Ochoa s/n, E-18071 Granada, Spain.
authors.forename: Francisco
authors.initials: F
authors.lastname: Olmo
authors.affiliation: Departamento de Parasitología, Universidad de Granada, Severo Ochoa s/n, E-18071 Granada, Spain.
authors.forename: Clotilde
authors.initials: C
authors.lastname: Marín
authors.affiliation: Departamento de Parasitología, Universidad de Granada, Severo Ochoa s/n, E-18071 Granada, Spain.
authors.forename: Guillermo
authors.initials: G
authors.lastname: Chaves-Lemaur
authors.affiliation: Departamento de Estadística, Universidad de Granada, Severo Ochoa s/n, E-18071 Granada, Spain.
authors.forename: Ramón
authors.initials: R
authors.lastname: Gutierrez-Sánchez
authors.affiliation: Departamento de Parasitología, Universidad de Granada, Severo Ochoa s/n, E-18071 Granada, Spain. Electronic address: msanchem@ugr.es.
authors.forename: Manuel
authors.initials: M
authors.lastname: Sánchez-Moreno
mesh_terms: D000818:Animals; D014355:Chagas Disease / Q000188:drug therapy / Q000469:parasitology*; D002522:Chlorocebus aethiops; D005110:Extracellular Space / Q000187:drug effects / Q000469:parasitology; D005260:Female; D020128:Inhibitory Concentration 50; D042541:Intracellular Space / Q000187:drug effects / Q000469:parasitology; D007892:Leishmania braziliensis / Q000187:drug effects; D018314:Leishmania infantum / Q000187:drug effects; D007896:Leishmaniasis / Q000188:drug therapy / Q000469:parasitology*; D051379:Mice; D008958:Models, Molecular; D008968:Molecular Conformation; D009942:Organometallic Compounds / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D028561:Transition Elements / Q000737:chemistry*; D014230:Triazoles / Q000737:chemistry*; D014344:Trypanocidal Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use / Q000633:toxicity; D014349:Trypanosoma cruzi / Q000187:drug effects; D014709:Vero Cells
chemical_list: D009942:Organometallic Compounds; D028561:Transition Elements; D014230:Triazoles; D014344:Trypanocidal Agents
keywords: Leishmania; Metal; Triazolopyrimidine; Trypanosoma cruzi