SYNTHESIS AND LEISHMANICIDAL ACTIVITY OF NEW BIS-ALKYLQUINOLINES

Bis-alkylquinolines 1-6 were synthetized via Williamson reaction between 8-hydroxyquinaldine with different É, ù-dihaloalkanes. Structures of all the products were elucidated by spectroscopic analysis. Cytotoxic and antileishmanial activities of synthesized compounds were determinated on U-937 cells...

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Veröffentlicht in:Journal of the Chilean Chemical Society 2013, Vol.58 (2), p.1709-1712
Hauptverfasser: CARDONA, WILSON, ARANGO, VICTOR, DOMÍNGUEZ, JORGE J, ROBLEDO, SARA M, MUÑOZ, DIANA L, FIGADERE, BRUNO, VELEZ, IVAN D, SÁEZ, JAIRO
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Sprache:eng
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Zusammenfassung:Bis-alkylquinolines 1-6 were synthetized via Williamson reaction between 8-hydroxyquinaldine with different É, ù-dihaloalkanes. Structures of all the products were elucidated by spectroscopic analysis. Cytotoxic and antileishmanial activities of synthesized compounds were determinated on U-937 cells and L. (V) panamensis amastigotes, respectively. Compound 5, 1,9-bis[(2-methylquinolin-8-yl)oxy]nonane, was the most selective against axenic and intracellular amastigotes (EC50 = 11.3 and 22.6, ìg/mL), with selectivity indices greater than 17.7 and 8.8, respectively; which makes this compound promising for the developing of new leishmanicidal drugs.
ISSN:0717-9707
0717-9707
DOI:10.4067/S0717-97072013000200014