Applied Natural Product Chemistry
Our research targets are biologically active natural organic compounds. Using synthetic organic chemistry, we aim to elucidate the mechanism of activity expression and structure-activity relationship of physiologically active substances, and to apply them to agricultural chemicals and medicines.
Overview: Synthesis and activity evaluation of natural organic compounds and analogues, Elucidation of biosynthetic pathways of physiologically active substances, Application of biocatalysts (microorganisms and enzymes) to organic synthesis, Development of useful organic reactions
Target: antibiotics, plant pathogenic toxins, plant hormones, anorexia, insect attractants; repellents, aroma substances
Development: anticancer agents, antitumor agents, antiviral agents (influenza, novel coronavirus, HIV), herbicides, antibiotics, insecticides, perfumeries
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X-ray crystal analysis of the covalent bond complex (fluorosialic acid-influenza sialidase)
There is an urgent need to develop anti-influenza drugs following Tamiflu. We have elucidated the mechanism of action of influenza sialidase by irreversibly inhibiting this enzyme by 2,3-difluorosialic acid 1. Furthermore, as a next-generation inhibitor, we synthesized sulfosialic acid derivative 2 with the aim of increasing affinity with the enzyme active center, and showed that the introduction of a sulfo group is effective for new lead development.
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Glycans have attracted much attention as molecules that play various roles in biological recognition, but their detailed functions are still unknown due to their structural complexity and diversity. Therefore, we are investigating efficient synthetic methods for glycans and glycoconjugate derivatives, including the use of enzymes as well as chemical methods. We are also constructing a compound library of alkaloids and heterocyclic compounds, and searching for anti-nematode drugs against pine bark beetles (one of the causes of pine wilt).