کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1376563 | 981961 | 2008 | 5 صفحه PDF | دانلود رایگان |

Five tacrine–ferulic acid hybrids (6a–e) were designed and synthesized as multi-potent anti-Alzheimer drug candidates. All target compounds have better acetylcholinesterase inhibitory activity and comparable butyrylcholinesterase inhibitory activity in relation to tacrine. Interestingly, 6d showed a reversible and non-competitive inhibitory action for acetylcholinesterase indicating interaction with the peripheral anionic site, whereas a reversible but competitive inhibitory action for butyrylcholinesterase. The antioxidant study revealed that four target compounds have, compared to Trolox, high ability to absorb reactive oxygen species.
Novel ChE inhibitory (IC50: AChE 4.4–38.6 nM; BChE 5.9–34.1 nM) and antioxidant (0.4–2.0 equiv to Trolox) tacrine–ferulic acid hybrids are reported.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 9, 1 May 2008, Pages 2905–2909