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

被引：54

作者：

Caballero, Ana B. ^{[1
]}

Rodriguez-Dieguez, Antonio ^{[1
]}

Quiros, Miguel ^{[1
]}

Salas, Juan M. ^{[1
]}

Huertas, Oscar ^{[2
]}

Ramirez-Macias, Inmaculada ^{[2
]}

Olmo, Francisco ^{[2
]}

Marin, Clotilde ^{[2
]}

Chaves-Lemaur, Guillermo ^{[2
]}

Gutierrez-Sanchez, Ramon ^{[3
]}

Sanchez-Moreno, Manuel ^{[2
]}

机构：

[1] Univ Granada, Dept Quim Inorgan, E-18071 Granada, Spain

[2] Univ Granada, Dept Parasitol, E-18071 Granada, Spain

[3] Univ Granada, Dept Estadist, E-18071 Granada, Spain

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 85卷

关键词：

Metal; Triazolopyrimidine; Leishmania; Trypanosoma cruzi; IN-VITRO ACTIVITY; TRYPANOSOMA-CRUZI; TROPICAL DISEASES; ANTITUMOR-ACTIVITY; PLATINUM(II) COMPLEXES; BIOLOGICAL-ACTIVITY; NICKEL-COMPLEXES; DRUGS; CHEMOTHERAPY; DERIVATIVES;

D O I：

10.1016/j.ejmech.2014.08.026

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 Dypanosoma 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. (C) 2014 Elsevier Masson SAS. All rights reserved.

引用

页码：526 / 534

页数：9

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