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Biomedical subjects

Tatsuhiro Harada

Publications and source records attributed to Tatsuhiro Harada.

2 recordsLinked to original sources

2,3-Diphenylpropionic acids as potent VLA-4 antagonists.

The discovery and SAR of 2,3-diphenylpropionic acid derivatives as highly potent VLA-4 antagonists are described. One representative compound, 9cc has inhibited intercellular adhesion by a VCAM-1/VLA-4 interaction with an IC(50) of 1.7 nM, and has good pharmacokinetics and oral bioavailability.

Administration, Oral↗

Reverse hydroxamate-based selective TACE inhibitors.

Reverse hydroxamate-based selective TACE inhibitors are described. They have potent TACE inhibitory activities and excellent selectivities against MMP-1, 2, 3, 8, 9, 13, 14, and 17. One representative compound, 18 has demonstrated an excellent oral inhibitory activity of the lipopolysaccharide (LPS)-stimulated TNF-alpha production in rats.

ADAM Proteins↗