کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1370067 981807 2016 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Antileishmanial activity of novel indolyl–coumarin hybrids: Design, synthesis, biological evaluation, molecular docking study and in silico ADME prediction
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Antileishmanial activity of novel indolyl–coumarin hybrids: Design, synthesis, biological evaluation, molecular docking study and in silico ADME prediction
چکیده انگلیسی

In present work we have designed and synthesized total twelve novel 3-(3-(1H-indol-3-yl)-3-phenylpropanoyl)-4-hydroxy-2H-chromen-2-one derivatives 13(a–l) using Ho3+ doped CoFe2O4 nanoparticles as catalyst and evaluated for their potential antileishmanial and antioxidant activities. The compounds 13a, 13d and 13h were found to possess significant antileishmanial activity (IC50 value = 95.50, 95.00 and 99.00 μg/mL, respectively) when compared to the standard sodium stibogluconate (IC50 = 490.00 μg/mL). The compounds 13a (IC50 = 12.40 μg/mL), 13d (IC50 = 13.49 μg/mL), 13g (IC50 = 13.24 μg/mL) and 13l (IC50 = 13.74 μg/mL) had shown good antioxidant activity when compared with standards butylated hydroxy toluene (IC50 = 16.5 μg/mL) and ascorbic acid (IC50 = 12.8 μg/mL). After performing molecular docking studies, it was found that compounds 13a and 13d had potential to inhibit pteridine reductase 1 enzyme. In silico ADME pharmacokinetic parameters had shown promising results and none of the synthesized compounds had violated Lipinski’s rule of five. Thus, suggesting that compounds from the present series can serve as important gateway for the design and development of new antileishmanial as well as antioxidant agent.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 3, 1 February 2016, Pages 829–835
نویسندگان
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