筑波大学WPI-IIIS長瀬研究室(創薬化学)では、オレキシン作動薬の開発やオピオイドの研究を行っています。

2014 Original Papers / 2014 原著論文

  1. Watanabe, Y.; Kitazawa, S.; Fujii, H.; Nemoto, T.; Hirayama, S.; Iwai, T.; Gouda, H.; Hirono, S.; Nagase, H.
    “Design, synthesis, and structure-activity relationship of novel opioid κ receptor selective agonists: α-Iminoamide derivatives with an azabicyclo[2.2.2]octene skeleton”
    Bioorg. Med. Chem. Lett. 2014, 24, 4980-4983. (web)
  2. Nozaki, C.; Nagase, H.; Nemoto, T.; Matifas, A.; Kieffer, B. L.; Gaveriaux-Ruff, C.
    In vivo properties of KNT-127, a novel delta opioid agonist: receptor internalisation, antihyperalgesia and antidepressant effects in mice”
    Br. J. Pharmacol. 2014, 171, 5376-5386. (web)
  3. Hirayama, S.; Wada, N.; Kuroda, N.; Iwai, T.; Yamaotsu, N.; Hirono, S.; Fujii, H.; Nagase, H.
    “Synthesis of a novel universal opioid receptor agonist with the 1,3,5-trioxazatriquinane skeleton and its pharmacologies”
    Bioorg. Med. Chem. Lett. 2014, 24, 4895-4898. (web)
  4. Hirayama, S.; Wada, N.; Nemoto, T.; Iwai, T.; Fujii, H.; Nagase, H.
    “Synthesis and Pharmacology of a Novel κ Opioid Receptor (KOR) Agonist with a 1,3,5-Trioxazatriquinane Skeleton”
    ACS Med. Chem. Lett. 2014, 5, 868-872. (web)
  5. Kutsumura, N.; Toguchi, S.; Iijima, M.; Tanaka, O.; Iwakura, I.; Saito, T.
    “DBU-promoted regioselective HBr-elimination of vicinal dibromides: effects of the adjacent oxygen and/or other heterofunctional groups”
    Tetrahedron 2014, 70, 8004-8009. (web)
  6. Saito, T.; Sonoki, Y.; Otani, T.; Kutsumura, N.
    “Triflic acid-promoted cycloisomerization of 2-alkynylphenyl isothiocyanates and isocyanates: a novel synthetic method for a variety of indole derivatives”
    Org. Biomol. Chem. 2014, 12, 8398-8407. (web)   Front Cover
  7. Kubo, H.; Matsui, K.; Saitoh, T.; Nishiyama, S.
    “Synthesis and assignment of the absolute stereochemistry of (+)-hemifistularin 3″
    Tetrahedron 2014, 70, 6392-6397. (web)
  8. Kashiwagi, T; Fuchigami, T; Saitoh, T; Nishiyama, S; Atobe, M.
    “Sequential paired electrosynthesis of a diary ether derivative using an electrochemical micro reactor”
    Chem. Lett. 2014, 43, 799-801. (web)
  9. Nagase, H.; Nakajima, R.; Yamamoto, N.; Hirayama, S.; Iwai, T.; Nemoto, T.; Gouda, H.; Hirono, S.; Fujii, H.
    “Design and synthesis of quinolinopropellane derivatives with selective δ opioid receptor agonism”
    Bioorg. Med. Chem. Lett. 2014, 24, 2851-2854. (web)
  10. Kardon, A. P.; Polgar, E.; Hachisuka, J.; Snyder, L. M.; Cameron, D., Savage, S.; Cai, X.; Karnup, S.; Fan, C. R.; Hemenway, G. M.; Bernard, C. S.; Schwartz, E. S.; Nagase, H.; Schwarzer, C.; Watanabe, M.; Furuta, T.; Kaneko, T.; Koerber, H. R.; Todd, A. J.; Ross, S. E.
    “Dynorphin Acts as a Neuromodulator to Inhibit Itch in the Dorsal Horn of the Spinal Cord”
    Neuron 2014, 82, 573-586. (web)
  11. Sugiyama, A.; Nagase, H.; Oka, J.; Yamada, M.; Saitoh, A.
    “DOR2-selective but not DOR1-selective antagonist abolishes anxiolytic-like effects of the delta opioid receptor agonist KNT-127″
    Neuropharmacology 2014, 79, 314-320. (web)
  12. Fujii, H.; Hayashida, K.; Saitoh, A.; Yokoyama, A.; Hirayama, S.; Iwai, T.; Nakata, E.; Nemoto, T.; Sudo, Y.; Uezono, Y.; Yamada, M.; Nagase, H.
    “Novel Delta Opioid Receptor Agonists with Oxazatricyclodecane Structure”
    ACS Med. Chem. Lett. 2014, 5, 368-372. (web)
  13. Kawa, K.; Saitoh, T.; Kaji, E.; Nishiyama, S.
    “Glycosylation of a Newly Functionalized Orthoester Derivative”
    Molecules 2014, 19, 2602-2611. (web)
  14. Ishikawa, K.; Tomatsu, M.; Nagase, H.; Fujii, H.
    “Zinc-acetic acid promoted reductive carbon-nitrogen bond cleavage reaction of α-aminoketones”
    Heterocycles 2014, 88, 1051-1063. (web)
  15. Kawabata, Y.; Naito, Y.; Saitoh, T.; Kawa, K.; Fuchigami, T.; Nishiyama, S.
    “Synthesis of (+)-O-Methylthalibrine Employing a Stereocontrolled Bischler-Napieralski Reaction and an Electrochemically Generated Diaryl Ether”
    Eur. J. Org. Chem. 2014, 99-104. (web)

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筑波大学WPI-IIIS長瀬研究室(創薬化学)では、オレキシン作動薬の開発や、オピオイドの研究を行っています。

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