In Vitro and in Vivo Trypanocidal Evaluation of Nickel Complexes with an Azapurine Derivative against <i>Trypanosoma cruzi</i>

Maldonado, Carmen R.; Marı́n, Clotilde; Olmo, F.J.; Huertas, Óscar; Quirós, Miguel; Sánchez‐Moreno, Manuel; Rosales, María J.; Salas, Juan M.

doi:10.1021/jm100581z

Cited by 25 publications

(7 citation statements)

References 35 publications

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“…Chagas' disease is caused by the protozoan Trypanosoma cruzi ( T. cruzi ) that affects a lot of people in Latin America . The current available drugs such as nifurtimox or benznidazole are only effective against the acute phase, but exhibit very limited efficacy in the chronic stage and even have high toxicity and severe side effect.…”

Section: Imidazoles As Antiparasitic Agentsmentioning

confidence: 99%

Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry

et al. 2013

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Imidazole ring is an important five-membered aromatic heterocycle widely present in natural products and synthetic molecules. The unique structural feature of imidazole ring with desirable electron-rich characteristic is beneficial for imidazole derivatives to readily bind with a variety of enzymes and receptors in biological systems through diverse weak interactions, thereby exhibiting broad bioactivities. The related research and developments of imidazole-based medicinal chemistry have become a rapidly developing and increasingly active topic. Particularly, numerous imidazole-based compounds as clinical drugs have been extensively used in the clinic to treat various types of diseases with high therapeutic potency, which have shown the enormous development value. This work systematically gives a comprehensive review in current developments of imidazole-based compounds in the whole range of medicinal chemistry as anticancer, antifungal, antibacterial, antitubercular, anti-inflammatory, antineuropathic, antihypertensive, antihistaminic, antiparasitic, antiobesity, antiviral, and other medicinal agents, together with their potential applications in diagnostics and pathology. It is hoped that this review will be helpful for new thoughts in the quest for rational designs of more active and less toxic imidazole-based medicinal drugs, as well as more effective diagnostic agents and pathologic probes.

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Section: Imidazoles As Antiparasitic Agentsmentioning

confidence: 99%

Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry

et al. 2013

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“…4,[19][20][21] The combination of metal ions with drugs and organic ligands can enhance their activity while at the same time, reducing the toxicity and undesired side effects that metal ions on their own could impart. [22][23][24] In this study, the synthesis of a series of amino-and iminopyridyl ligands and some of their metal complexes is reported. In addition, their anti-parasitic activity against L. amazonensis promastigotes and T. cruzi trypomastigotes is evaluated.…”

Section: Introductionmentioning

confidence: 99%

Glycosylated metal chelators as anti-parasitic agents with tunable selectivity

et al. 2017

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Trypanosoma cruzi and Leishmania amazonensis are the causative agents of Chagas' disease and leishmaniasis, respectively. These conditions affect millions of people worldwide, especially in developing countries. As such, there is an urgent need for novel, efficient and cost-effective treatments for these diseases, given the growing resistance and side-effects of current therapies. This work details the synthesis and evaluation of the anti-parasitic activity of novel amino- and iminopyridyl metal chelators, their glycosylated derivatives and some of their metal complexes. Our results revealed the potent and metal-dependent activity for the aminopyridyl compounds: Cu(ii) complexes were most effective against T. cruzi trypomastigotes, while Zn(ii) complexes presented excellent activity against L. amazonensis promastigotes. In addition, the compounds showed excellent selectivity indexes and very low relative toxicity as judged by in vitro and in vivo studies, respectively, using RAW macrophages and Galleria mellonella larvae model.

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“…Compared with purines, the fused-ring system of these ligands differs only in the presence of a pyrimidine nitrogen atom in a bridgehead position and the disappearance of the acidic H-proton of the five-membered ring [6,7]. Furthermore, these bicyclic heterocycles have been subjected to chemical and biological tests due to their pharmacological properties, including anticancer [8,9], antibacterial [10], antiviral [11], anti-inflammatory [12,13], fungicidal [14], antiparasitic [15][16][17][18][19] and leishmanicidal properties [20][21][22][23][24].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, characterization and in vitro cytotoxicity of three types of platinum(II) complexes containing 5,7-diethyl-1,2,4-triazolo[1,5-a]pyrimidine

Łakomska

Babinska

Wojtczak

et al. 2016

Inorganica Chimica Acta

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In Vitro and in Vivo Trypanocidal Evaluation of Nickel Complexes with an Azapurine Derivative against Trypanosoma cruzi

Cited by 25 publications

References 35 publications

Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry

Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry

Glycosylated metal chelators as anti-parasitic agents with tunable selectivity

Synthesis, characterization and in vitro cytotoxicity of three types of platinum(II) complexes containing 5,7-diethyl-1,2,4-triazolo[1,5-a]pyrimidine

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