کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1392347 1501131 2014 9 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Triazolopyrimidine compounds containing first-row transition metals and their activity against the neglected infectious Chagas disease and leishmaniasis
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Triazolopyrimidine compounds containing first-row transition metals and their activity against the neglected infectious Chagas disease and leishmaniasis
چکیده انگلیسی


• Six new metal complexes bearing 5,7-dimethyl-1,2,4-triazolo[1,5-a]pyrimidine.
• Similar toxicity than reference drugs against two different Leishmania and Trypanosoma cruzi.
• Less toxic and much more selective towards parasite than reference drugs.
• In vivo studies against T. cruzi display lesser parasitemia than the control.
• Described compounds may be considered as potential agents against trypanosomatids.

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.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 85, 6 October 2014, Pages 526–534
نویسندگان
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