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542.05:615.31:616.98:575.821HIV (1) |
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SM ISO690:2012 BILAN, Dmitri, MACAEV, Fliur. Agenţii noi anti-HIV pe bază de isatină, sclareol şi leucină. In: Revista de Ştiinţă, Inovare, Cultură şi Artă „Akademos”, 2019, nr. 4(55), pp. 44-51. ISSN 1857-0461. DOI: https://doi.org/10.5281/zenodo.3631301 |
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Revista de Ştiinţă, Inovare, Cultură şi Artă „Akademos” | |||||
Numărul 4(55) / 2019 / ISSN 1857-0461 /ISSNe 2587-3687 | |||||
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DOI: https://doi.org/10.5281/zenodo.3631301 | |||||
CZU: 542.05:615.31:616.98:575.821HIV | |||||
Pag. 44-51 | |||||
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Synthesis of optic active hybrid compounds derivatives of oxindole has been performed via condensation of isatin with photosensible p-acetoazobenzene and transformational products of sclareol and leucine. It has been demonstrated that cytotoxicity of the sesquiterpenoide derivatives based on (+)-sclareol diminishes at change from the fife-membered lactamic ring to diole, as wellas at at the chage of nature of the bicyclic fragment, while increases at the change from the multisubstituted derivative of oxindole with a pyrrole fragment. The lowest cytotxicity has been detected for acetoacetate 11, which is comparable to that of the azoderivative 4а with values CC50 (cytotoxicity concentration 50 %) 0.0315 and CC50 = 0.0301 mМ, respectively, while the hybrid compound based on leucine has a twice lower toxicity (CC50 0.0116 mМ). It has been established that the compound 5а has affected the human immunodeficiency virus (HIV) replication at 24 times lower concentrations IC50 (inhibitory concentration 50 %) 0.0031 mМ than the antiretroviral agent didanosine (IC50 0.075 mМ), a reverstranscriptase inhibitor used in the HIV therapy. |
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Cuvinte-cheie isatin, diterpenoide sclareol, leucine, Citotoxicity, anti-HIV, isatină, diterpenoidă sclareol, leucină, citotoxicitate, anti-HIV |
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