2013 Fiscal Year Final Research Report
Design and Synthesis of Chloroalkene Dipeptide Isosteres as Ground State Peptidomimetics for drug discovery
| Project/Area Number |
24790107
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Drug development chemistry
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| Research Institution | Shizuoka University (2013)
Tokyo Medical and Dental University (2012) |
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Principal Investigator |
NARUMI Tetsuo 静岡大学, 工学(系)研究科(研究院), 准教授 (50547867)
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| Project Period (FY) |
2012-04-01 – 2014-03-31
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| Keywords | アミド結合等価体 |
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| Research Abstract |
As part of a program aimed at acceleration of the peptide-lead drug discovery, synthetic studies and a structural analysis of a newly designed dipeptide bioisosteres possessing an E/Z-chloroalkene unit as the surrogate functionality of a peptide bond were investigated. In this study, practical and divergent methodologies for the synthesis of chloroalkenes dipeptide isosteres (CADIs) have been developed including large-scale synthesis of Xaa-Gly-type CADIs and highly diastereoselective synthesis of Xaa-Xaa-type CADIs. These studies should contribute to the development of alkene dipeptide isosteres-based medicinal chemistry.
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[Journal Article] A CD4 Mimic as an HIV Entry Inhibitors : Pharmacokinetic2013
Author(s)
Hashimoto, C.; Nar umi, T.; Otsuki, H.; Hirota, Y.; Arai, H.; Yoshimura, K.; Harada, S.; Ohashi, N.; Nomura, W.; Miura, T.; Igarashi, T.; Matsushita S.; Tamamura, H., Bioorg
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Journal Title
Med. Chem
Volume: 21(24)
Pages: 7884-7889
Peer Reviewed
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[Journal Article] Generation of a Replication-competent Simian-human Immunodeficiency Virus, the Neutralisation Sensitivity of Which can be Enhanced in the Presence of a Small Molecule CD4 Mimic2013
Author(s)
Otsuki, H.; Hishiki, T.; Miura, T.; Hashimoto, C.; Nar umi, T.; Tamamura, H.; Yoshimura, K.; Matsushita, S.; Igarashi, T
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Journal Title
J. Gen. Virol
Volume: 94(12)
Pages: 2710-2716
Peer Reviewed
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[Journal Article] Low Molecular Weight CXCR4 Ligands with Variable Spacers2013
Author(s)
Nar umi, T.; Aikawa, H.; Tanaka, T.; Hashimoto, C.; Ohashi, N., Nomura, W.; Kobayakawa, T.; Takano, H.; Hirota, Y.; Murakami, T.; Yamamoto, N.; Tamamura, H
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Journal Title
ChemMedChem
Volume: 8(1)
Pages: 118-124
Peer Reviewed
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[Journal Article] CD4 Mimics as HIV Entry Inhibitors : Lead Optimization Studies of the Aromatic Substituents2013
Author(s)
Nar umi, T.; Arai, H.; Yoshimura, K.; Harada, S.; Hirota, Y.; Ohashi, N.; Hashimoto, C.; Nomura, W.; Matsushita, S.; Tamamura, H
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Journal Title
Bioorg. Med. Chem
Volume: 21(9)
Pages: 2518-2526
Peer Reviewed
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[Journal Article] Conjugation of Cell-penetrating Peptides Leads to Identification of Anti-HIV Peptides from Matrix Proteins2013
Author(s)
Nar umi, T.; Komoriya, M.; Hashimoto, C.; Wu, H.; Nomura, W.; Suzuki, S.; Tanaka, T.; Chiba, J.; Yamamoto, N.; Murakami, T.; Tamamura, H., Bioorg
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Journal Title
Med. Chem
Volume: 20(4)
Pages: 1468-1474
Peer Reviewed
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[Journal Article] Synthetic C34 Trimer of HIV-1 gp41 Shows Significant Increase of Inhibition Potency2012
Author(s)
Nomura, W.; Hashimoto, C.; Ohya, A.; Miyauchi, K.; Urano, E.; Tanaka, T.; Nar umi, T., Nakahara, T.; Komano, J. A.; Yamamoto, N.; Tamamura, H
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Journal Title
ChemMedChem
Volume: 7(2)
Pages: 205-208
Peer Reviewed
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[Journal Article] Pharmacophore-Based Small Molecule CXCR4 Ligands2012
Author(s)
Nar umi, T.; Tanaka, T.; Hashimoto, C.; Nomura, W.; Aikawa, H.; Sohma, A.; Itotani, K.; Kawamata, M.; Murakami, T.; Yamamoto, N.; Tamamura, H
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Journal Title
Bioorg. Med. Chem. Lett
Volume: 22(12)
Pages: 4169-4172
Peer Reviewed
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