1333383-62-2Relevant articles and documents
Synthesis and Evaluation of Antimalarial Activity of Oxygenated 3-alkylpyridine Marine Alkaloid Analogues
Hilario, Flaviane F.,de Paula, Renata Cristina,Silveira, Mariana L. T.,Viana, Gustavo H. R.,Alves, Rosemeire B.,Pereira, Juliana R.C.S.,Silva, Luciana Maria,de Freitas, Rossimiriam P.,de Pilla Varotti, Fernando
, p. 477 - 482 (2011)
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.
Effect of 3-Alkylpyridine Marine Alkaloid Analogues in Leishmania Species Related to American Cutaneous Leishmaniasis
Machado, Patricia A.,Carvalho, Lidiane O.,Coimbra, Elaine S.,Hilario, Flaviane F.,Silveira, Mariana L. T.,Alves, Rosemeire B.,Freitas, Rossimiriam P.
, p. 745 - 751,7 (2012)
A series of oxygenated analogues of marine 3-alkylpyridine alkaloids were synthesized, and their leishmanicidal activity was assayed. All compounds were prepared from 3-pyridinepropanol in few steps and in good yields. The key step for the synthesis of these compounds was a classic Williamson etherification under phase-transfer conditions. Besides toxicity in peritoneal macrophages, the compounds exhibited a significant leishmanicidal activity. Of twelve compounds tested, five showed a strong leishmanicidal activity against promastigote forms of Leishmania amazonensis and L. braziliensis with IC50 below 10μm. Compounds 11, 14, 15, and 16 showed a strong leishmanicidal activity on intracellular amastigotes (IC50 values of 2.78; 0.27; 1.03, and 1.33μm, respectively), which is unlikely to be owing to the activation of nitric oxide production by macrophages.
