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pubmed:abstractText |
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(i) of 6nM and represents a novel class of reversible, highly potent and non-peptidic calpain inhibitors.
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pubmed:affiliation |
Department of CNS Discovery Research, Abbott GmbH&Co. KG, PO Box 210805, 67008, Ludwigshafen, Germany. wilfried.lubish@abbott.com
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