Design and synthesis of 4-aryl-4-oxobutanoic acid amides as calpain inhibitors |
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| Authors: | Yong Zhang Seo Yoon Jung Changbae Jin Nam Doo Kim Ping Gong Yong Sup Lee |
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| Institution: | 1. School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang 110016, Liaoning, PR China;2. Department of Pharmaceutical Science, College of Pharmacy & Department of Life and Nanopharmaceutical Science, Kyung Hee University, 1 Hoegi-dong Dongdaemoon-ku, Seoul 130-701, Republic of Korea;3. Doping Control Center, Korea Institute of Science & Technology, Seoul 130-650, Republic of Korea;4. R&D Center, Equispharm Company, Limited, Sungnam, Kyunggi-do 463-825, Republic of Korea |
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| Abstract: | The involvement of μ-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 μ-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 μ-calpain (IC50 = 0.34 μM). Our findings suggest that the 4-aryl-4-oxobutanoic acid amide derivatives should be considered as a new family of μ-calpain inhibitors. |
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