Synthesis and evaluation of antimalarial activity of oxygenated 3-alkylpyridine marine alkaloid analogues.
| Autor: | Hilário FF; Departamento de Química, ICEx, UFMG, Av. Pres. Antonio Carlos, 6627, Pampulha, Belo Horizonte, MG, 31270-901, Brazil., de Paula RC, Silveira ML, Viana GH, Alves RB, Pereira JR, Silva LM, de Freitas RP, de Pilla Varotti F |
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| Jazyk: | angličtina |
| Zdroj: | Chemical biology & drug design [Chem Biol Drug Des] 2011 Sep; Vol. 78 (3), pp. 477-82. Date of Electronic Publication: 2011 Jul 08. |
| DOI: | 10.1111/j.1747-0285.2011.01154.x |
| Abstrakt: | A series of new oxygenated analogues of marine 3-alkylpyridine alkaloids were prepared from 3-pyridinepropanol in few steps and in good yields. The key step for the synthesis of these compounds was a Williamson etherification under phase-transfer conditions. All new compounds were evaluated for their antiplasmodial activity and cytotoxicity. A significant reduction in parasitaemia was observed for some of the prepared compounds, and the majority of them exhibited a selectivity index (SI) ranging from 2.78 to 15.58, which suggests that these compounds may be a promising class of substances with antimalarial activity. (© 2011 John Wiley & Sons A/S.) |
| Databáze: | MEDLINE |
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