Byeon, Seong Rim Kim, Hyunjin Vincent Jeon, Mijin Ahn, Young Gil Kim, Maeng Sup Kong, Jae Yang Kim, Hye Yun Kim, Young Soo Kim, Dong Jin 2024-01-20T12:04:07Z 2024-01-20T12:04:07Z 2022-01-10 2013-06-01 0960-894X https://pubs.kist.re.kr/handle/201004/127976 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-beta. 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 mu M) results indicated safety of KMS80013. (C) 2013 Elsevier Ltd. All rights reserved. English Pergamon Press Ltd. SOLID-PHASE SYNTHESIS CURCUMIN DRUG HYPOTHESIS PATHOLOGY PEPTIDE Therapeutic and pharmacokinetic characterizations of an anti-amyloidogenic bis-styrylbenzene derivative for Alzheimer's disease treatment Article 10.1016/j.bmcl.2013.02.104 1 Bioorganic & Medicinal Chemistry Letters, v.23, no.11, pp.3467 - 3469 Bioorganic & Medicinal Chemistry Letters 23 11 3467 3469 scie scopus 000318976100070 2-s2.0-84877586188 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article SOLID-PHASE SYNTHESIS CURCUMIN DRUG HYPOTHESIS PATHOLOGY PEPTIDE Amyloid-beta Alzheimer&apos s disease Aggregation inhibitor Pharmacokinetics Behavior test