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discovery of an orally bioavailable benzofuran analogue that serves as a β-amyloid aggregation inhibitor for the potential treatment of alzheimer's disease
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نویسنده
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ha h.-j. ,kang d.w. ,kim h.-m. ,kang j.-m. ,ann j. ,hyun h.j. ,lee j.h. ,kim s.h. ,kim h. ,choi k. ,hong h.-s. ,kim y. ,jo d.-g. ,lee j. ,lee j.
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منبع
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journal of medicinal chemistry - 2018 - دوره : 61 - شماره : 1 - صفحه:396 -402
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چکیده
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We developed an orally active and blood-brain-barrier-permeable benzofuran analogue (8, mdr-1339) with potent antiaggregation activity. compound 8 restored cellular viability from aβ-induced cytotoxicity but also improved the learning and memory function of ad model mice by reducing the aβ aggregates in the brains. given the high bioavailability and brain permeability demonstrated in our pharmacokinetic studies, 8 will provide a novel scaffold for an aβ-aggregation inhibitor that may offer an alternative treatment for ad.
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آدرس
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sungkyunkwan university, school of pharmacy, south korea, seoul national university, laboratory of medicinal chemistry, south korea, seoul national university, college of pharmacy, laboratory of medicinal chemistry, south korea, seoul national university, college of pharmacy, laboratory of medicinal chemistry, south korea, seoul national university, college of pharmacy, laboratory of medicinal chemistry, south korea, sungkyunkwan university, school of pharmacy, south korea, sungshin university, department of global medical science, south korea, seoul national university, laboratory of medicinal chemistry, south korea
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Authors
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