Therapeutic and pharmacokinetic characterizations of an anti-amyloidogenic bis-styrylbenzene derivative for Alzheimer's disease treatment
- Therapeutic and pharmacokinetic characterizations of an anti-amyloidogenic bis-styrylbenzene derivative for Alzheimer's disease treatment
- 변성림; 김현진; 전미진; 안영길; 김맹섭; 공재양; 김혜연; 김영수; 김동진
- amyloid; Alzheimer's disease; Alzheimer; 치매; 알츠하이머병; 아밀로이드; Aggregation inhibitor; Pharmacokinetics; Behavior test; Amyloid-β
- Issue Date
- Bioorganic & medicinal chemistry letters
- VOL 23, NO 11, 3467-3469
- Alzheimer’s disease drug discovery regarding exploration into the molecules and processes has focused on the intrinsic causes of the brain disorder correlated with the accumulation of amyloid-b. An anti-amyloidogenic bis-styrylbenzene derivative, KMS80013, showed excellent oral bioavailability (F = 46.2%), facilitated brain penetration (26%, iv) in mouse and target specific in vivo efficacy in acute AD mouse model attenuating the cognitive deficiency in Y-maze test. Acute toxicity (LD50 >2000 mg/kg) and hERG channel inhibition (14% at 10 lM) results indicated safety of KMS80013.
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