کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1395334 1501204 2009 9 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Phase transfer catalyzed synthesis of bis-quinolines: Antileishmanial activity in experimental visceral leishmaniasis and in vitro antibacterial evaluation
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Phase transfer catalyzed synthesis of bis-quinolines: Antileishmanial activity in experimental visceral leishmaniasis and in vitro antibacterial evaluation
چکیده انگلیسی

A one-pot synthesis of some novel bis-quinolines has been achieved under phase transfer catalyzed conditions using 8-hydroxy quinoline derivatives as substrates. The synthesized analogues were evaluated for antileishmanial activity against Leishmania donovani promastigotes and amastigotes. The entire bis-quinolines showed efficacy in both in vitro and in vivo studies. Compound 5 (1,1-bis-[(5-chloro-8-quinolyl)oxy]methane) exhibited the most significant activity. Compounds 4 (1,1-bis-[(8-quinolyl)oxy]methane) and 9 (1,5-bis-[(2-methyl-8-quinolyl)oxy]pentane) also demonstrated significant leishmanicidal efficacy against established visceral leishmaniasis in BALB/c model. Ultrastructural studies of promastigotes treated with compound 5, demonstrated membrane blebbing, chromatin condensation and vacuolization in the parasites and the flagellated parasites became round shaped after treatment. Moreover, in vitro antibacterial activity of compound 5 against several bacterial strains revealed its promising efficacy. The findings suggested that 1,1-bis-[(5-chloro-8-quinolyl)oxy]methane (5) is a bright candidate to be considered as lead compound for leishmanicidal drug.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 44, Issue 2, February 2009, Pages 845–853
نویسندگان
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