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Medicinal chemistry studies based on the three-dimensional structural diversity-oriented molecular design of pharmacologically active compounds

Research Project

Project/Area Number 15H02495
Research Category

Grant-in-Aid for Scientific Research (A)

Allocation TypeSingle-year Grants
Section一般
Research Field Drug development chemistry
Research InstitutionHokkaido University

Principal Investigator

Shuto Satoshi  北海道大学, 薬学研究院, 教授 (70241346)

Co-Investigator(Kenkyū-buntansha) 小松 康雄  国立研究開発法人産業技術総合研究所, 生命工学領域, 研究グループ付 (30271670)
福田 隼  長崎大学, 医歯薬学総合研究科(薬学系), 准教授 (30434450)
有澤 光弘  大阪大学, 薬学研究科, 准教授 (40312962)
山口 浩明  東北大学, 大学病院, 助教 (80400373)
一ノ瀬 亘  北海道大学, 薬学研究科(研究院), 特別研究員 (00636409)
Project Period (FY) 2015-04-01 – 2020-03-31
Project Status Completed (Fiscal Year 2019)
Budget Amount *help
¥41,080,000 (Direct Cost: ¥31,600,000、Indirect Cost: ¥9,480,000)
Fiscal Year 2018: ¥8,450,000 (Direct Cost: ¥6,500,000、Indirect Cost: ¥1,950,000)
Fiscal Year 2017: ¥9,230,000 (Direct Cost: ¥7,100,000、Indirect Cost: ¥2,130,000)
Fiscal Year 2016: ¥9,230,000 (Direct Cost: ¥7,100,000、Indirect Cost: ¥2,130,000)
Fiscal Year 2015: ¥14,170,000 (Direct Cost: ¥10,900,000、Indirect Cost: ¥3,270,000)
Keywordsシクロプロパン / 三次元多様性 / レゾルビン / ヌクレオシド / ペプチドミメティクス / ライブラリー / ペプチドミイメティクス
Outline of Final Research Achievements

Based on the three-dimensional structural diversity-oriented strategy using characteristic structural features of cyclopropane, medicinal chemistry studies have been carried out. As the result of these studies, various pharmacologically active compounds, such as, highly active congeners of pro-resolving lipid mediator RvE2, peptidomimetics including prorenin inhibitors and melanocortin receptor-4 selective ligands, membrane-permeable cyclic peptides, or the first GABA transporter GAT1-selective inhibitor, were identified. Thus, it was demonstrated that the three-dimensional structural diversity-oriented strategy effectively works for the theoretical development of desired pharmacologically active compounds. In addition, various synthetic procedures for the substituted chiral cyclopropanes, which can be effectively used in cyclopropane medicinal chemistry studies, have been developed.

Academic Significance and Societal Importance of the Research Achievements

企業とアカデミアの創薬科学は、それぞれ「生産性」と「論理性」を鍵として相互補完的関係であることが望ましく、このような相互補完性がもたらす相乗効果が、創薬の科学としての、また産業としての発展をもたらす。本研究成果は、所望の標的分子に選択的に結合する化合物を偶然 (スクリーニング) に依存することなく、効率的かつ論理的に創出する方法論を提示するものであり、アカデミアとしての創薬化学研究として、学術的のみならず社会的にも大きな意義がある。

Report

(5 results)
  • 2019 Final Research Report ( PDF )
  • 2018 Annual Research Report
  • 2017 Annual Research Report
  • 2016 Annual Research Report
  • 2015 Annual Research Report
  • Research Products

    (54 results)

All 2019 2018 2017 2016 2015 Other

All Int'l Joint Research (2 results) Journal Article (38 results) (of which Int'l Joint Research: 5 results,  Peer Reviewed: 38 results,  Acknowledgement Compliant: 16 results,  Open Access: 8 results) Presentation (11 results) (of which Int'l Joint Research: 5 results,  Invited: 3 results) Remarks (1 results) Patent(Industrial Property Rights) (2 results)

  • [Int'l Joint Research] University of Copenhagen(デンマーク)

    • Related Report
      2018 Annual Research Report
  • [Int'l Joint Research] コペンハーゲン大学(デンマーク)

    • Related Report
      2017 Annual Research Report
  • [Journal Article] Synthesis of Enantiomerically Pure 1,2,3-Trisubstituted Cyclopropane Nucleosides Using Pd-Catalyzed Substitution via Directing Group-Mediated C(sp3)?H Activation as a Key Step2019

    • Author(s)
      Minami Takaaki、Fukuda Kohtaro、Hoshiya Naoyuki、Fukuda Hayato、Watanabe Mizuki、Shuto Satoshi
    • Journal Title

      Organic Letters

      Volume: 21 Issue: 3 Pages: 656-659

    • DOI

      10.1021/acs.orglett.8b03785

    • Related Report
      2018 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Development of a Highly Potent Analogue and a Long-Acting Analogue of Oxytocin for the Treatment of Social Impairment-Like Behaviors2019

    • Author(s)
      Ichinose W, Cherepanov SM, Shabalova AA, Yokoyama S, Yuhi T, Yamaguchi H, Watanabe A, Yamamoto Y, Okamoto H, Horike S, Terakawa J, Daikoku T, Watanabe M, Mano N, Higashida H, Shuto S
    • Journal Title

      J Med Chem

      Volume: - Issue: 7 Pages: 3297-3310

    • DOI

      10.1021/acs.jmedchem.8b01691

    • Related Report
      2018 Annual Research Report
    • Peer Reviewed / Int'l Joint Research
  • [Journal Article] Ligand-Phospholipid Conjugation: a Versatile Strategy for Developing Long-Acting Ligands that Bind to Membrane Proteins by Restricting the Subcellular Localization of the Ligand2018

    • Author(s)
      Kawamura, Y. Ito, T. Hirokawa, E. Hikiyama, S. Yamada, S. Shuto
    • Journal Title

      J. Med. Chem.

      Volume: 61 Issue: 9 Pages: 4020-4029

    • DOI

      10.1021/acs.jmedchem.8b00041

    • Related Report
      2018 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Synthesis of Chiral cis-Cyclopropane Bearing Indole and Chromone as Potential TNFα Inhibitors2018

    • Author(s)
      Kanada Ryutaro、Tanabe Makoto、Muromoto Ryuta、Sato Yukina、Kuwahara Tomoki、Fukuda Hayato、Arisawa Mitsuhiro、Matsuda Tadashi、Watanabe Mizuki、Shuto Satoshi
    • Journal Title

      The Journal of Organic Chemistry

      Volume: 83 Issue: 15 Pages: 7672-7682

    • DOI

      10.1021/acs.joc.8b00466

    • Related Report
      2018 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Resolvin E1, but not resolvins E2 and E3, promotes fMLF-induced ROS generation in human neutrophils2018

    • Author(s)
      Unno Yuka、Sato Yoshinori、Fukuda Hayato、Ishimura Kohei、Ikeda Hiroyuki、Watanabe Mizuki、Tansho-Nagakawa Shigeru、Ubagai Tsuneyuki、Shuto Satoshi、Ono Yasuo
    • Journal Title

      FEBS Letters

      Volume: 592 Issue: 16 Pages: 2706

    • DOI

      10.1002/1873-3468.13215

    • Related Report
      2018 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Resolvin E3 attenuates lipopolysaccharide-induced depression-like behavior in mice2018

    • Author(s)
      Deyama Satoshi、Shimoda Kento、Ikeda Hiroyuki、Fukuda Hayato、Shuto Satoshi、Minami Masabumi
    • Journal Title

      Journal of Pharmacological Sciences

      Volume: 138 Issue: 1 Pages: 86-88

    • DOI

      10.1016/j.jphs.2018.09.006

    • NAID

      120006540074

    • Related Report
      2018 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Design and synthesis of cyclopropane-based conformationally restricted GABA analogues as selective inhibitors for betaine/GABA transporter 12018

    • Author(s)
      Suemasa Akihiro、Watanabe Mizuki、Kobayashi Takaaki、Suzuki Hiroe、Fukuda Hayato、Minami Masabumi、Shuto Satoshi
    • Journal Title

      Bioorganic & Medicinal Chemistry Letters

      Volume: 28 Issue: 20 Pages: 3395-3399

    • DOI

      10.1016/j.bmcl.2018.08.031

    • Related Report
      2018 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Development of dihydrodibenzooxepine PPAR gamma ligands of a novel binding mode as anticancer agents: Effective mimicry of chiral structures by olefinic E/Z-isomers2018

    • Author(s)
      Yamamoto, T. Tamura, K. Henmi, T. Kuboyama, A. Yanagisawa, M. Matsubara, Y. Takahashi, M. Suzuki, J. Saito, K.Ueno, S. Shuto
    • Journal Title

      J. Med. Chem.

      Volume: 61 Issue: 22 Pages: 10067-10083

    • DOI

      10.1021/acs.jmedchem.8b01200

    • Related Report
      2018 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Design and Synthesis of Histamine H3/H4 Receptor Ligands with a Cyclopropane Scaffold. Bioorg2018

    • Author(s)
      Watanabe, T. Kobayashi, Y. Ito, H. Fukuda, S. Yamada, M. Arisawa, S. Shuto,
    • Journal Title

      Bioorg. Med. Chem. Lett

      Volume: 28 Pages: 3630-3633

    • Related Report
      2018 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Highly Conformationally-Restricted Cyclopropane Tethers with three-Dimensional Structural Diversity Drastically Enhance the Cell-Permeability of Cyclic Peptides2017

    • Author(s)
      K. Matsui, Y. Kido, R. Watari, Y. Kashima, Y. Yoshida, S. Shuto
    • Journal Title

      Chem. Eur. J.

      Volume: 23 Issue: 13 Pages: 1-9

    • DOI

      10.1002/chem.201604946

    • Related Report
      2017 Annual Research Report 2016 Annual Research Report
    • Peer Reviewed
  • [Journal Article] From Peptides to Peptidomimetics: A Strategy Based on the Structural Features of Cyclopropane2017

    • Author(s)
      Mizuno Akira、Matsui Kouhei、Shuto Satoshi
    • Journal Title

      Chemistry - A European Journal

      Volume: 23 Issue: 58 Pages: 14394-14409

    • DOI

      10.1002/chem.201702119

    • Related Report
      2017 Annual Research Report
    • Peer Reviewed
  • [Journal Article] An Entry to Chiral 1,1,2,3-Tetrasubstituted Arylcyclopropanes by Pd(II)-Catalyzed Arylation via Directing Group-Mediated C(sp3)-H Activation.2017

    • Author(s)
      N. Hoshiya, M. Kondo, H. Fukuda, M. Arisawa, J. Uenishi, S. Shuto
    • Journal Title

      J. Org. Chem.

      Volume: 82 Issue: 5 Pages: 2535-2544

    • DOI

      10.1021/acs.joc.6b02935

    • Related Report
      2017 Annual Research Report 2016 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] M. Minami, Resolvin E1 and E2 ameliorate lipopolysaccharide-induced depression-like behaviors via ChemR232017

    • Author(s)
      K. Deyama, Y. Shimoda, K. Ishikawa, H. Ishimura, H. Fukuda, S. Ide, M. Satoh, S. Shuto
    • Journal Title

      Psychopharmacology

      Volume: 235 Issue: 1 Pages: 329-336

    • DOI

      10.1007/s00213-017-4774-7

    • Related Report
      2017 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Structure-specific Effects of Lipidated Oxytocin Analogs on Intracellular Calcium Levels, Parental Behavior, Plasma and Cerebrospinal Fluid Oxytocin Concentrations in Mice.2017

    • Author(s)
      S. M. Cherepanov, S. Yokoyama, A. Mizuno, W. Ichinose, O. Lopatina, A. A. Shabalova, A. B. Salmina, Y. Yamamoto, H. Okamoto, S. Shuto, H. Higashida
    • Journal Title

      Pharmacol. Res. Perspect.

      Volume: 5 Issue: 1 Pages: 1-14

    • DOI

      10.1002/prp2.290

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Discovery of Novel Seven-Membered Prostacyclin Analogs as Potent and Selective Prostaglandin FP and EP3 Dual Agonists.2017

    • Author(s)
      I. Sugimoto, T. Kambe, T. Okino, T. Obitsu, N. Ohta, T. Nishiyama, A. Kinoshita, T. Fujimoto, H. Egashira, S.Yamane, S. Shuto, K.Tani, T. Maruyama
    • Journal Title

      ACS Med. Chem. Lett.

      Volume: 8 Issue: 1 Pages: 107-112

    • DOI

      10.1021/acsmedchemlett.6b00415

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Cyclopropane-Based Peptidomimetics Mimicking Wide-Ranging Secondary Structures of Peptides: Conformational Analysis and Their Use in Rational Ligand Optimization.2017

    • Author(s)
      A. Mizuno, T. Kameda, T. Kuwahara, H. Endoh, Y. Ito, S. Yamada, K. Hasegawa, A. Yamano, M. Watanabe, M. Arisawa, S. Shuto
    • Journal Title

      Chem. Eur. J.

      Volume: 23 Issue: 13 Pages: 3159-3168

    • DOI

      10.1002/chem.201605312

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Discovery of Novel Indazole Derivatives as Orally Available β3-Adrenergic Receptor Agonists Lacking Off-Target-Based Cardiovascular Side Effect.2017

    • Author(s)
      Y. Wada, S. Nakano, A. Morimoto, K. Kasahara, T. Hayash, Y. Takada, H. Suzuki, M. NIwa-Sakai, S. Ohashi, M. Mori, T. Hirokawa, S. Shuto
    • Journal Title

      J. Med. Chem.

      Volume: 60 Issue: 8 Pages: 3252-3265

    • DOI

      10.1021/acs.jmedchem.6b01197

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Pd(II)-Catalyzed Alkylation of Tertiary Carbon via Directing Group-Mediated C(sp3)-H Activation: Synthesis of Chiral 1,1,2-Trialkylsubstituted Cyclopropane.2016

    • Author(s)
      N. Hoshiya, K. Takenaka, S. Shuto, J. Uenishi
    • Journal Title

      Org. Lett

      Volume: 18 Issue: 1 Pages: 48-51

    • DOI

      10.1021/acs.orglett.5b03229

    • Related Report
      2016 Annual Research Report 2015 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Identification of Adenine and Benzimidazole Nucleosides as Potent Human Concentrative Nucleoside Transporter 2 Inhibitors: Potential Treatment for Hyperuricemia and Gout.2016

    • Author(s)
      K. Tatani, M. Hiratochi, N. Kikuchi, Y. Kuramochi, S. Watanabe, Y. Yamauchi, M. Isaji, S, Shuto
    • Journal Title

      J. Med. Chem

      Volume: 59 Issue: 8 Pages: 3719-3731

    • DOI

      10.1021/acs.jmedchem.5b01884

    • Related Report
      2016 Annual Research Report 2015 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Non-metathesis Heterocycle Formation by Ruthenium-Catalyzed Intramolecular [2+2] Cycloaddition of Allenamide-enes to Azabicyclo[3.1.1]heptanes2016

    • Author(s)
      Tomomi Nada, Yusuke Yoneshige, Yasuhiro Ii, Takashi Matsumoto, Hiromichi Fujioka, Satoshi Shuto, Mitsuhiro Arisawa
    • Journal Title

      ACS Catalysis

      Volume: 6 Issue: 5 Pages: 3168-3171

    • DOI

      10.1021/acscatal.6b00628

    • Related Report
      2016 Annual Research Report 2015 Annual Research Report
    • Peer Reviewed / Open Access / Acknowledgement Compliant
  • [Journal Article] Self-assembled Multi-layer Stabilized Nickel Nanoparticle Catalyst for Ligand-free Cross-coupling Reactions: in situ Metal Nanoparticle and Nanospace Simultaneous Organization2016

    • Author(s)
      Naoyuki Hoshiya, Katsumasa Fujiki, Takahisa Taniguchi, Tetsuo Honma, Yusuke Tamenori, Mincen Xiao, Nozomi Saito, Mami Yokoyama, Akira Ishii, Hiromichi Fujioka, Satoshi Shuto, Yoshihiro Sato, Mitsuhiro Arisawa
    • Journal Title

      Adv. Synth. Catal.

      Volume: 358 Issue: 15 Pages: 2449-2459

    • DOI

      10.1002/adsc.201600024

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed / Int'l Joint Research / Acknowledgement Compliant
  • [Journal Article] Design, Synthesis, and Identification of 4α-azidoethyl-Cyclic ADP-Carbocyclic-Ribose as a Highly Potent Analogue of Cyclic ADP-Ribose a Ca2+-mobilizing Second Messenger2016

    • Author(s)
      Sato, T.; Watanabe, M.; Tsuzuki, T.; Takano, S.; Murayama, T.; Sakurai, T.; Kameda, T.; Arisawa, M.; Fukuda, H.; Shuto, S.
    • Journal Title

      J. Med. Chem.

      Volume: 59 Issue: 15 Pages: 7282-7286

    • DOI

      10.1021/acs.jmedchem.6b00437

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Development of a Sulfur-Modified Glass-Supported Pd Nanoparticle Catalyst for Suzuki–Miyaura Coupling2016

    • Author(s)
      Mincen Xiao, Naoyuki Hoshiya, Katsumasa Fujiki, Tetsuo Honma, Yusuke Tamenori, Satoshi Shuto, Hiromichi Fujioka, Mitsuhiro Arisawa
    • Journal Title

      Chemical and Pharmaceutical Bulletin

      Volume: 64 Issue: 8 Pages: 1154-1160

    • DOI

      10.1248/cpb.c16-00261

    • NAID

      130005253911

    • ISSN
      0009-2363, 1347-5223
    • Related Report
      2016 Annual Research Report
    • Peer Reviewed / Open Access / Acknowledgement Compliant
  • [Journal Article] Design and Synthesis of Cyclopropane Congeners of Resolvin E2, an Endogenous Proresolving Lipid Mediator, as Its Stable Equivalents2016

    • Author(s)
      Fukuda, H; Muromoto, R.; Takakura, Y.; Ishimura, K.; Kanada, R.; Fushihara, D.; Tanabe, M.; Matsubara, K.; Hirao, T.; Hirashima, K.; Abe, Arisawa, M.; Matsuda, T.; Shuto, S.
    • Journal Title

      Org. Lett.

      Volume: 18 Issue: 24 Pages: 6224-6227

    • DOI

      10.1021/acs.orglett.6b02612

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed / Int'l Joint Research / Acknowledgement Compliant
  • [Journal Article] Novel Characteristics of Guanosine 5’-monophosphate 1 Reductase in Pathogenic2 Protozoa Trypanosoma brucei Distinct from Host Animal.2016

    • Author(s)
      T. Bessho, T. Okada, C. Kimura, T. Shinohara, A. Tomiyama, A. Imamura, M. Kuwamura, K. Nishimura, K. Fujimori, .S. Shuto, O. Ishibashi, B. K. Kubata, T. Inui
    • Journal Title

      PLoS Negl. Trop. Dis

      Volume: 10 Issue: 1 Pages: e0004339-e0004339

    • DOI

      10.1371/journal.pntd.0004339

    • Related Report
      2015 Annual Research Report
    • Peer Reviewed / Open Access / Int'l Joint Research
  • [Journal Article] Identification of a Potent and Selective GPR4 Antagonist as a Drug Lead for the Treatment of Myocardial Infarction2016

    • Author(s)
      Hayato Fukuda, Saki Ito, Kenji Watari, Chihiro Mogi, Mitsuhiro Arisawa, Fumikazu Okajima, Hitoshi Kurose, Satoshi Shuto
    • Journal Title

      ACS Med. Chem. Lett.

      Volume: 7 Issue: 5 Pages: 493-497

    • DOI

      10.1021/acsmedchemlett.6b00014

    • Related Report
      2015 Annual Research Report
    • Peer Reviewed / Open Access / Acknowledgement Compliant
  • [Journal Article] Lipo-oxytocin-1, A Novel Oxytocin Analog Conjugated with Two Palmitoyl Groups, Has Long-lasting Effects on Anxiety-related Behavior and Social Avoidance in CD157 Knockout Mice.2015

    • Author(s)
      A. Mizuno, S. M. Cherepanov, Y. Kikuchi, A. Fakhrul, S. Akther, K. Deguchi, T. Yoshihara, K. Ishihara, S. Shuto , H. Higashida
    • Journal Title

      Brain Sci

      Volume: 5 Issue: 1 Pages: 3-13

    • DOI

      10.3390/brainsci5010003

    • Related Report
      2015 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Determination of ω-6 and ω-3 PUFA metabolites in human urine samples using UPLC/MS/MS.2015

    • Author(s)
      A. Sasaki, H. Fukuda, N. Shiida, N. Tanaka, A. Furugen, J. Ogura, S. Shuto, N. Mano, H. Yamaguchi
    • Journal Title

      Anal. Bioanal. Chem

      Volume: 407 Issue: 6 Pages: 1625-1639

    • DOI

      10.1007/s00216-014-8412-5

    • Related Report
      2015 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Identification of 8-Aminoadenosine Derivatives as a New Class of Human Concentrative Nucleoside Transporter 2 Inhibitors.2015

    • Author(s)
      K. Tatani, M. Hiratochi, Y. Nonaka, M. Isaji, S. Shuto
    • Journal Title

      ACS Med. Chem. Lett

      Volume: 6 Issue: 3 Pages: 244-248

    • DOI

      10.1021/ml500343r

    • Related Report
      2015 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Nickel-Catalyzed Suzuki-Miyaura Coupling of a Tertiary Iodocyclopropane with Wide Boronic Acid Substrate Scope: Coupling Reaction Outcome Depends on Radical Species Stability2015

    • Author(s)
      Keisuke Yotsuji, Naoyuki Hoshiya, Takaaki Kobayashi, Hayato Fukuda, Hiroshi Abe, Mitsuhiro Arisawa and Satoshi Shuto
    • Journal Title

      Adv. Synth. Catal.

      Volume: 357 Issue: 5 Pages: 1022-1028

    • DOI

      10.1002/adsc.201401000

    • Related Report
      2015 Annual Research Report
    • Peer Reviewed / Open Access / Acknowledgement Compliant
  • [Journal Article] Double Carbonylation of Aryl Iodides with Amines under an Atmospheric Pressure of Carbon Monoxide Using Sulfur- Modified Au-Supported Palladium2015

    • Author(s)
      Nozomi Saito Takahisa Taniguchi, Naoyuki Hoshiya, Satoshi Shuto, Mitsuhiro Arisawa, Yoshihiro Sato
    • Journal Title

      Green Chem.

      Volume: 17 Issue: 4 Pages: 2358-2361

    • DOI

      10.1039/c4gc02469a

    • Related Report
      2015 Annual Research Report
    • Peer Reviewed / Open Access / Acknowledgement Compliant
  • [Journal Article] Characterization of imidazopyridine compounds as negative allosteric modulators of proton-sensing GPR4 in extracellular acidification-induced responses2015

    • Author(s)
      Ayaka Tobo, Masayuki Tobo, Takashi Nakakura, Masashi Ebara, Hideaki Tomura, Chihiro Mogi, Dong-Soon Im, Naoya Murata, Atsushi Kuwabara, Saki Ito, Hayato Fukuda, Mitsuhiro Arisawa, Satoshi Shuto, Michio Nakaya, Hitoshi Kurose, Koichi Sato, Fumikazu Okajima
    • Journal Title

      PLoS One.

      Volume: 10 Issue: 6 Pages: e0129334-e0129334

    • DOI

      10.1371/journal.pone.0129334

    • Related Report
      2015 Annual Research Report
    • Peer Reviewed / Open Access / Int'l Joint Research / Acknowledgement Compliant
  • [Journal Article] Construction of a chiral quaternary carbon center by a radical cyclization/ring-enlargement reaction: synthesis of 4α-azidoethyl carbocyclic ribose, a key unit for the synthesis of cyclic ADP- ribose derivatives of biological importance2015

    • Author(s)
      Takatoshi Sato, Takayoshi Tsuzuki, Satoshi Takano, Kohtaro Kato, Hayato Fukuda, Mitsuhiro Arisawa, Satoshi Shuto
    • Journal Title

      Tetrahedron

      Volume: 71 Issue: 33 Pages: 5407-5413

    • DOI

      10.1016/j.tet.2015.05.084

    • Related Report
      2015 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Synthesis of 7-Deaza-cyclic Adenosine-5′-diphosphate-carbocyclic-ribose and Its 7-Bromo Derivative as Intracellular Ca2+-Mobilizing Agents2015

    • Author(s)
      Satoshi Takano, Takayoshi Tsuzuki, Takashi Murayama, Takashi Sakurai, Hayato Fukuda, Mitsuhiro Arisawa, Satoshi Shuto
    • Journal Title

      J. Org. Chem.

      Volume: 80 Issue: 13 Pages: 6619-6627

    • DOI

      10.1021/acs.joc.5b00723

    • Related Report
      2015 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Discovery of Novel Indazole Derivatives as Highly Potent and Selective Human β3-Adrenergic Receptor Agonists without Cardiovascular Side Effects.2015

    • Author(s)
      Y. Wada, H. Shirahashi, T. Iwanami, M. Ogawa, S. Nakano, A. Morimoto, K. Kasahara, E. Tanaka, Y. Takada, S. Ohashi, M. Mori, S. Shuto
    • Journal Title

      J. Med. Chem

      Volume: 58 Issue: 15 Pages: 6048-6057

    • DOI

      10.1021/acs.jmedchem.5b00638

    • Related Report
      2015 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Safe Removal of the Allyl Protecting Groups of Allyl Esters using a Recyclable, Low-leaching and Ligand-free Palladium Nanoparticle Catalyst2015

    • Author(s)
      Koji Takagi, Hayato Fukuda, Satoshi Shuto, Akira Otaka, Mitsuhiro Arisawa
    • Journal Title

      Adv. Synth. Catal.

      Volume: 357 Issue: 9 Pages: 2119-2124

    • DOI

      10.1002/adsc.201500055

    • Related Report
      2015 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Rolling Circle Translation of Circular RNA in Living Human Cells.2015

    • Author(s)
      N. Abe, K. Matsumoto, M. Nishihara, Y. Nakano, A. Shibata, H. Maruyama, S. Shuto, A. Matsuda, M. Yoshida, Y. Ito, H. Abe
    • Journal Title

      Scientific Rep

      Volume: 15 Issue: 1 Pages: 16435-16435

    • DOI

      10.1038/srep16435

    • Related Report
      2015 Annual Research Report
    • Peer Reviewed / Open Access
  • [Journal Article] One-pot Olefin Isomerization/ Aliphatic Enamine Ring-closing Metathesis/ Oxidation/ 1,3-Dipolar Cycloaddition for the Synthesis of Isoindolo[1,2-a]isoquinolines2015

    • Author(s)
      Yuki Fujii, Tsunayoshi Takehara, Takeyuki Suzuki, Hiromichi Fujioka, Satoshi Shuto, Mitsuhiro Arisawa
    • Journal Title

      Adv. Synth. Catal.

      Volume: 357 Issue: 18 Pages: 4055-4062

    • DOI

      10.1002/adsc.201500680

    • Related Report
      2015 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Presentation] GABAトランスポーターサブタイプ選択的阻害剤の創出を目的とするGABA配座制限誘導体の設計と合成2018

    • Author(s)
      末政亮大、中田和彰、小林嵩明、福田隼、渡邉瑞貴、井手聡一郎、人羅菜津子、南雅文、周東智
    • Organizer
      日本薬学会第138年会
    • Related Report
      2017 Annual Research Report
  • [Presentation] trans-1, 2-シクロプロパンジアミンおよびジカルボン酸からなるオリゴアミドの合成研究2018

    • Author(s)
      山田 圭恭, 一ノ瀬 亘, 福田 隼, 渡邉 瑞貴, 周東智
    • Organizer
      日本薬学会 第138年会
    • Related Report
      2017 Annual Research Report
  • [Presentation] シクロプロパンの構造特性に基づく膜透過性環状ペプチドの設計と合成2018

    • Author(s)
      植村 真衣, 加藤 七海,松井 耕平, 桑原 智希, 渡邉 瑞貴, 福田 隼, 竹内 恒, 広川 貴次, 武隈 洋, 菅原 満, 周東 智
    • Organizer
      日本薬学会第138年会
    • Related Report
      2017 Annual Research Report
  • [Presentation] Rational Development of Cyclopropane-Based Target-Selective Compounds such as GABA Transporter Inhibitors2017

    • Author(s)
      周東智
    • Organizer
      Drug Research Academy
    • Related Report
      2017 Annual Research Report
    • Int'l Joint Research / Invited
  • [Presentation] 炎症収束性脂質レゾルビンE1配座制限誘導体の設計と合成2017

    • Author(s)
      石村 航平,福田 隼,渡邉 瑞貴,周東 智
    • Organizer
      第15回次世代を担う有機化学シンポジウム
    • Related Report
      2017 Annual Research Report
  • [Presentation] 光学活性1,2,3-三置換シクロプロパンヌクレオシドの合成2017

    • Author(s)
      南貴覚、福多洸太朗、星谷尚亨、福田隼、渡邉瑞貴、周東智
    • Organizer
      第29回万有札幌シンポジウム
    • Related Report
      2017 Annual Research Report
  • [Presentation] Spiro-cyclopropane type α-helix/β-strand mimimetics targeting protein-protein interactions2017

    • Author(s)
      Tomoki Kuwahara, Akira Mizuno, Hayato Fukuda, Mizuki Watanabe, Satoshi Shuto
    • Organizer
      254th ACS National Meeting & Exposition
    • Related Report
      2017 Annual Research Report
    • Int'l Joint Research
  • [Presentation] Development of Conformationally Restricted Peptides and Peptidomimetics Based on the Structural Features of Cyclopropane2017

    • Author(s)
      渡邉瑞貴
    • Organizer
      The 3rd HU-TMU-KU Joint Symposium for Pharmaceutical Sciences
    • Related Report
      2017 Annual Research Report
    • Int'l Joint Research
  • [Presentation] シクロプロパンの立体及び立体電子特性に基づくペプチドミメティクス2017

    • Author(s)
      桑原智希,植村真衣,水野彰,一ノ瀬亘,松井耕平,福田隼,渡邉瑞貴,周東智
    • Organizer
      第43回反応と合成の進歩シンポジウム
    • Related Report
      2017 Annual Research Report
  • [Presentation] Design and Synthesis of Biologically Active Compounds Based on the Structural Features of Cyclopropane2016

    • Author(s)
      Satoshi Shuto
    • Organizer
      The 8th Takeda Science Foundation Symposium on Pharmasciences. Biomolecule-Based Medicinal Science: Featuring Mid-Size Drugs
    • Place of Presentation
      武田薬品工業研究所(大阪府吹田市)
    • Year and Date
      2016-01-21
    • Related Report
      2015 Annual Research Report
    • Int'l Joint Research / Invited
  • [Presentation] Medicinal chemical study on cyclic ADP‐ribose for developing the stable and potent agonists and antagonists2015

    • Author(s)
      Satoshi Shuto
    • Organizer
      FASEB Science Research Conference on NAD Metabolism and Signaling
    • Place of Presentation
      Timmendorfer Strand, Germany
    • Year and Date
      2015-08-09
    • Related Report
      2015 Annual Research Report
    • Int'l Joint Research / Invited
  • [Remarks] 創薬有機化学研究室ホームページ

    • URL

      https://www.pharm.hokudai.ac.jp/yuuki/index.html

    • Related Report
      2018 Annual Research Report
  • [Patent(Industrial Property Rights)] プロレニン受容体リガンド及びアンタゴニスト2016

    • Inventor(s)
      周東 智、石田 晋、神田敦宏、桑原智希
    • Industrial Property Rights Holder
      周東 智、石田 晋、神田敦宏、桑原智希
    • Industrial Property Rights Type
      特許
    • Industrial Property Number
      2016-023315
    • Filing Date
      2016-02-10
    • Related Report
      2015 Annual Research Report
  • [Patent(Industrial Property Rights)] 環状ペプチドの膜透過性および/または代謝安定性を改善するシクロプロパンアミノ酸ユニット2015

    • Inventor(s)
      松井耕平、周東 智
    • Industrial Property Rights Holder
      松井耕平、周東 智
    • Industrial Property Rights Type
      特許
    • Industrial Property Number
      2015-167408
    • Filing Date
      2015-08-27
    • Related Report
      2015 Annual Research Report

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Published: 2015-04-16   Modified: 2022-11-04  

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