24(I-10) Recent Development in the Synthesis and Bio-Screening of the Natural-Originated Compounds
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概要
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Recently, our interests focus on the synthesis and the bio-screening of the natural-originated compounds in enantio-pure form on the basis of the new developed synthetic methods in this group. In this presentation, the synthesis and evaluation of the biologically active compounds are illustrated by the on-going subjects. For example, in light of our recent discovery of Ni(0) catalyzed homo-coupling and cross-coupling reactions, together with consulting the therapeutic information of Chinese traditional medicine from plants, the screenings of the compounds obtained by the above mentioned reactions have been undertaken. The preliminary results showed that the phthalide-type compounds showed good neuroprotection activities, and the coumarinyl derivatives exhibited excellent anti-fungal effects. The second topic is on the GABA neurotransmitter. The GABA reuptake is effected by selective transporter called GAT-1. The reduction of GABAergic neuronal activity plays an important role in a number of neurological disorders, including epilepsy, auxiety and pain. Several designed compounds bearing with (R)-nipecotic acid moiety were synthesized and found very active in inhibiting GABA reuptake showing the possible usage for the analgesic chemotherapeutic treatment.
- 天然有機化合物討論会の論文
- 2004-10-01
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関連論文
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- 24(I-10) Recent Development in the Synthesis and Bio-Screening of the Natural-Originated Compounds