Discovery of an orally bioavailable benzofuran analogue that serves as a β-amyloid aggregation inhibitor for the potential treatment of Alzheimer's disease
HJ Ha, DW Kang, HM Kim, JM Kang… - Journal of Medicinal …, 2018 - ACS Publications
Journal of Medicinal Chemistry, 2018•ACS Publications
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.
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.
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.
ACS Publications
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