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Structure−Activity Relationship Study and Drug Profile of<i>N</i>-(4-Fluorophenylsulfonyl)-<scp>l</scp>-valyl-<scp>l</scp>-leucinal (SJA6017) as a Potent Calpain Inhibitor
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Description
Novel N-arylsulfonyldipeptidyl aldehyde derivatives were prepared by DMSO oxidation from the corresponding dipeptide alcohol, and their potencies as calpain inhibitors were evaluated in vitro. Among them, N-(4-fluorophenylsulfonyl)-l-valyl-l-leucinal (8, SJA6017) potently inhibited calpains. 8 also inhibited cathepsin B and L but did not inhibit other cysteine proteases (interleukin 1beta-converting enzyme), serine proteases (trypsin, chymotrypsin, thrombin, factor VIIa, factor Xa), or proteasome. Preliminary cytotoxicity studies of 8 exhibited a relatively safe profile.
Journal
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- Journal of Medicinal Chemistry
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Journal of Medicinal Chemistry 46 868-871, 2003-02-01
American Chemical Society (ACS)
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Keywords
- In Vitro Techniques
- Permeability
- Mice
- Structure-Activity Relationship
- Dogs
- Cytochrome P-450 Enzyme System
- Species Specificity
- Microsomes
- Toxicity Tests, Acute
- Animals
- Humans
- Protease Inhibitors
- Toxicity Tests, Chronic
- Cells, Cultured
- Calpain
- Blood Proteins
- Dipeptides
- Haplorhini
- Rats
- Hepatocytes
- Caco-2 Cells
Details 詳細情報について
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- CRID
- 1871710640956978304
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- ISSN
- 15204804
- 00222623
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- PubMed
- 12593666
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- Data Source
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- OpenAIRE