Antileishmanial activity of imidothiocarbamates and imidoselenocarbamates
| العنوان: | Antileishmanial activity of imidothiocarbamates and imidoselenocarbamates |
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| المؤلفون: | Daniel Plano, Juan Antonio Palop, Ylenia Baquedano, Carmen Sanmartín, David Moreno, Antonio Jiménez-Ruiz |
| المصدر: | Parasitology Research. 108:233-239 |
| بيانات النشر: | Springer Science and Business Media LLC, 2010. |
| سنة النشر: | 2010 |
| مصطلحات موضوعية: | Time Factors, Cell Survival, Antiprotozoal Agents, Pharmacology, Imides, Jurkat cells, Cell Line, Inhibitory Concentration 50, Selenium, chemistry.chemical_compound, Parasitic Sensitivity Tests, medicine, Humans, Leishmania infantum, Amastigote, IC50, Miltefosine, General Veterinary, biology, General Medicine, biology.organism_classification, In vitro, Infectious Diseases, chemistry, Mechanism of action, Insect Science, Parasitology, Carbamates, medicine.symptom, Edelfosine, medicine.drug |
| الوصف: | In the present study, a family of 15 imidothio- and imidoselenocarbamates (1-15) analogs have been synthesized and screened for their in vitro antileishmanial potential against Leishmania infantum promastigotes. The six most active ones (2, 4, 7, 13, 14, and 15) were also tested in an axenic amastigote model. In order to establish their selectivity indexes (SI) the cytotoxic effect of each compound was also assayed against Jurkat and THP-1 cell lines. Compounds 2 and 4, both with a pyridine moiety, showed a moderate antileishmanial activity with an IC(50) value of 4.68 ± 0.46 and 3.03 ± 0.24 μM, respectively, in the amastigote model. The activity was compared with that of standard drugs, edelfosine (IC₅₀ = 0.82 ± 0.13 μM) and miltefosine (IC₅₀ = 2.84 ± 0.10 μM). Related to selectivity, the SI of both compounds are similar to those of the standard drugs when compared against the THP-1 cell line. Moreover, compound 4 was able to reduce the number of amastigote-infected THP-1 cells to 40% of that observed in untreated controls after a 96-h period of treatment. These derivatives thus represent two new leads for further studies aimed at establishing their mechanism of action. |
| تدمد: | 1432-1955 0932-0113 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e3ab80bccb2ae9827190bb3110752874Test https://doi.org/10.1007/s00436-010-2073-xTest |
| حقوق: | CLOSED |
| رقم الانضمام: | edsair.doi.dedup.....e3ab80bccb2ae9827190bb3110752874 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 14321955 09320113 |
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