Artículos de revista (Inst. Salud Tropical)
Permanent URI for this collectionhttps://hdl.handle.net/10171/52056
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- Small molecules containing chalcogen elements (S, Se, Te) as new warhead to fight neglected tropical diseases(Elsevier, 2023) Sanmartin-Grijalba, C. (Carmen); Morán-Serradilla, C. (Cristina); Angulo-Elizari, E. (Eduardo); Plano-Amatriain, D. (Daniel); Henriquez-Figuereo, A. (Andreina)Neglected tropical diseases (NTDs) encompass a group of infectious diseases with a protozoan etiology, high incidence, and prevalence in developing countries. As a result, economic factors constitute one of the main obstacles to their management. Endemic countries have high levels of poverty, deprivation and marginalization which affect patients and limit their access to proper medical care. As a matter of fact, statistics remain un- collected in some affected areas due to non-reporting cases. World Health Organization and other organizations proposed a plan for the eradication and control of the vector, although many of these plans were halted by the COVID-19 pandemic. Despite of the available drugs to treat these pathologies, it exists a lack of effectiveness against several parasite strains. Treatment protocols for diseases such as American trypanosomiasis (Chagas disease), leishmaniasis, and human African trypanosomiasis (HAT) have not achieved the desired results. Un- fortunately, these drugs present limitations such as side effects, toxicity, teratogenicity, renal, and hepatic impairment, as well as high costs that have hindered the control and eradication of these diseases. This review focuses on the analysis of a collection of scientific shreds of evidence with the aim of identifying novel chalcogen- derived molecules with biological activity against Chagas disease, leishmaniasis and HAT. Compounds illustrated in each figure share the distinction of containing at least one chalcogen element. Sulfur (S), selenium (Se), and tellurium (Te) have been grouped and analyzed in accordance with their design strategy, chemical synthesis process and biological activity. After an exhaustive revision of the related literature on S, Se, and Te compounds, 183 compounds presenting excellent biological performance were gathered against the different causative agents of CD, leishmaniasis and HAT.
- Potential of sulfur-selenium isosteric replacement as a strategy for the development of new anti-chagasic drugs(2022) Alcolea-Devesa, V. (Verónica); Pérez-Silanes, S. (Silvia); Rubio-Hernández, M. (Mercedes)Current treatment for Chagas disease is based on only two drugs: benznidazole and nifurtimox. Compounds containing sulfur (S) in their structure have shown promising results in vitro and in vivo against Trypanosoma cruzi, the parasite causing Chagas disease. Notably, some reports show that the isosteric replacement of S by selenium (Se) could be an interesting strategy for the development of new compounds for the treatment of Chagas disease. To date, the activity against T. cruzi of three Se- containing groups has been compared with their S counterparts: selenosemicarbazones, selenoquinones, and selenocyanates. More studies are needed to confirm the positive results of Se compounds. Therefore, we have investigated S compounds described in the literature tested against T. cruzi. We focused on those tested in vivo that allowed isosteric replacement to propose their Se counterparts as promising compounds for the future development of new drugs against Chagas disease.
- Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity(Elsevier, 2016) Torres, E. (Enrique); Gonzalez, M. (Mercedes); Varela, J. (Javier); Arbillaga, L. (Leire); Pérez-Silanes, S. (Silvia); Moreno-de-Viguri, E. (Elsa); Cerecetto, H. (Hugo); Azqueta, A. (Amaya)Abstract: We report the synthesis and in vitro activity against T. cruzi epimastigotes of 15 novel quinoxaline derivatives. Ten of the derivatives presented IC50 values lower than the reference drugs Nfx and Bzn; four of them standed out with IC50 values lower than 1.5 M. Moreover, unspecific cytotoxicity and genotoxicity studies are also reported. Compound 14 showed a SI higher than 24, whereas compound 10 was the only one that was negative in the genotoxicity screening.
- Novel quinoxaline 1,4-di-N-oxide derivatives as new potential antichagasic agents(Elsevier, 2013-05-30) Devarapally, G. (Goutham); Aldana, I. (Ignacio); Torres, E. (Enrique); Gonzalez, M. (Mercedes); Varela, J. (Javier); Di-Maio, R. (Rossanna); Birriel, E. (Estefanía); Arbillaga, L. (Leire); Pérez-Silanes, S. (Silvia); Galiano, S. (Silvia); Monge, A. (Antonio); Moreno-de-Viguri, E. (Elsa); Cerecetto, H. (Hugo); Azqueta, A. (Amaya); Crawford, P.W. (Philip W.)As a continuation of our research and with the aim of obtaining new agents against Chagas disease, an extremely neglected disease which threatens 100 million people, eighteen new quinoxaline 1,4-di-Noxide derivatives have been synthesized following the Beirut reaction. The synthesis of the new derivatives was optimized through the use of a new and more efficient microwave-assisted organic synthetic method. The new derivatives showed excellent in vitro biological activity against Trypanosoma cruzi. Compound 17, which was substituted with fluoro groups at the 6- and 7-positions of the quinoxaline ring, was the most active and selective in the cytotoxicity assay. The electrochemical study showed that the most active compounds, which were substituted by electron-withdrawing groups,possessed a greater ease of reduction of the N-oxide groups