Synthesis and Anti-HIV Activity Evaluation of 2-(5-(Naphthalen-1-yl)-1,2,3-thiadiazol-4-ylthio)-N-acetamides Derivatives
The development of novel HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) offers the possibility of generating novel structures of increased potency. Based on the bioisosterism principle, two novel 2-(5-(naphthalen-1-yl)-1,2,3-thiadiazol-4-ylthio)-N-acetamides derivatives have been des...
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| Autores principales: | , , , |
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| Formato: | Articulo Comunicacion |
| Lenguaje: | Inglés |
| Publicado: |
2012
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| Materias: | |
| Acceso en línea: | http://sedici.unlp.edu.ar/handle/10915/20230 http://www.latamjpharm.org/resumenes/31/5/LAJOP_31_5_2_3.pdf |
| Aporte de: |
| Sumario: | The development of novel HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) offers the possibility of generating novel structures of increased potency. Based on the bioisosterism principle, two novel 2-(5-(naphthalen-1-yl)-1,2,3-thiadiazol-4-ylthio)-N-acetamides derivatives have been designed, synthesized and evaluated for their anti-HIV activities in MT-4 cells. The results indicate that these compounds show good activities against HIV-1. Especially, compound 9B (EC50 = 0.019 μM) was more effective than the reference drugs nevirapine and delavirdine. |
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