期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 12, 期 10, 页码 1335-1338出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(02)00176-2
关键词
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Novel calpain inhibitors derived from phenyl alanine aldehydes or ketoamides carrying a benzoyl residue were prepared and evaluated for their biological potency. A brief structure-activity relationship elucidated the importance of ortho-substitutents in the benzoyl moiety. The most potent derivative, the ketoamide 19c, exhibited a K, of 6 nM and represents a novel class of reversible, highly potent and non-peptidic calpain inhibitors. (C) 2002 Elsevier Science Ltd. All rights reserved.
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