URAMARU Naoto, Ph.D. / Senior Assistant Professor
Division of Pharmaceutical Health Biosciences
Department of Pharmaceutical Sciences
1. Design and synthesis based on metabolic activation of low-molecular-weight compounds.
2. Toxicology based on metabolic activation of environmental chemicals.
3. Research for traditional herbal medicines with anti-allergic activity.
Drug allergy is rare, but seriously and potentially lifethreatening. There are many reports that T-lymphocytes react specifically to low-molecular-weight compounds, even though peptide structures are required for antigen presentation. The reason for such hypersensitivity is that some low-molecular-weight drugs are metabolically activated and form complexes with proteins in vivo. We reported confirm the validity of our strategy of blocking metabolic activation of pyrazolones by means of structural modification to obtain compounds that can not be metabolically activated to bind to biomacromolecules and so do not show allergenicity but tetain potent antipyretic and analgesic activites. Research in our group is focused on medicinal chemistry on the design and synthesis based on metabolic activation of low-molecular-weight compounds.
1. Jiang W. P., Huang S. S., Matsuda Y., Saito H., Uramaru N., Ho H. Y., Wu J. B., Huang G. J., Protective effects of tormentic acid, a major component of suspension cultures of eriobotrya japonica cells, on acetaminophen induced hepatotoxicity in mice. Molecules, 22(5), 830 (2017).
2. Uramaru N., Inoue T., Watanabe Y., Shigematsu H., Ohta S., Kitamura S., Structure-activity relationship of a series of 17 parabens and related compounds for histamine release in rat peritoneal mast cells and skin allergic reaction in guinea pigs. Journal of Toxicological Sciences, 39, 83-90 (2014).
3. Uramaru N., Shigematsu H., Toda A., Eyanagi R., Kitamura S., Ohta S., Design, synthesis, and pharmacological activity of nonallergenic pyrazolone-type antipyretic analgesics. Journal of Medicinal Chemistry, 53, 8727-8733 (2010).