Zhang, Yong Jung, Seo Yoon Jin, Changbae Kim, Nam Doo Gong, Ping Lee, Yong Sup 2024-01-20T22:02:54Z 2024-01-20T22:02:54Z 2021-09-03 2009-01-15 0960-894X https://pubs.kist.re.kr/handle/201004/132802 The involvement of mu-calpain in neurological disorders, such as stroke and Alzheimer's disease has attracted considerable interest in the use of calpain inhibitors as therapeutic agents. 4-Aryl-4-oxobutanoic acid amide derivatives 4 were designed as acyclic variants of mu-calpain inhibitory chromone and quinolinone derivatives. Of the compounds synthesized, 4c-2, which possesses a 2-methoxymethoxy group at the phenyl ring and a primary amide at the warhead region most potently inhibited mu-calpain (IC50 = 0.34 mu M). Our findings suggest that the 4-aryl-4-oxobutanoic acid amide derivatives should be considered as a new family of mu-calpain inhibitors. (C) 2008 Elsevier Ltd. All rights reserved. English PERGAMON-ELSEVIER SCIENCE LTD CLEAVAGE Design and synthesis of 4-aryl-4-oxobutanoic acid amides as calpain inhibitors Article 10.1016/j.bmcl.2008.11.030 1 BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.19, no.2, pp.502 - 507 BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 19 2 502 507 scie scopus 000261908900047 2-s2.0-57749088398 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article CLEAVAGE Calpain inhibitor Stroke 4-Aryl-4-oxobutanoic acid Ketoamide Chromone