Rchr
J-GLOBAL ID:200901076277978010
Update date: Sep. 15, 2024
Haraguchi Kazuhiro
ハラグチ カズヒロ | Haraguchi Kazuhiro
Affiliation and department:
Job title:
Associate Professor
Research field (1):
Pharmaceuticals - chemistry and drug development
Research keywords (2):
有機合成化学
, Synthetic Organic Chemistry
Research theme for competitive and other funds (20):
- 2012 - 2015 Synthesis and evaluation of antiviral activities of branched oxetanosine A.
- 2009 - 2011 Synthesis of 4'-substtituted 4'-thionucleosides and evaluation of its biological activity
- 2007 - 2008 Regioselective Pummerer reacton of 4'-thionucleoside S-oxide : Synthesis of 1'-or 4'-substituted 4'-thionucleoside and its biological activity
- 2005 - 2006 Synthesis and Biological Activities of Sugar Modified 4'-Thionucleosides
- 2003 - 2004 Synthesis and Biological Activities of 4'-Thionucleosides branched at the Sugar Portion
- 1999 - 2000 チオフラノイドグリカールを利用する4'-チオヌクレオシドの立体選択的合成研究
- 1997 - 1998 共役ジエンの分子内オキシセレノ化反応を基盤とするオクトシルヌクレオシドの合成研究
- 1995 - 1995 ラジカル的アシルオキシ転位反応を基盤とする4'-炭素置換チミジンの立体選択的合成
- 1995 - 1995 ヌクレオシド糖部ラジカル反応における1,2-不斉誘起に関する研究
- 1994 - 1994 面選択的親電子付加反応を基盤とする1'-炭素置換ヌクレオシドの合成に関する研究
- 1994 - 1994 真正双頭ヌクレオシドの合成とその機能に関する研究
- 1993 - 1993 アリル転位に基づく立体選択的な4'-炭素置換ヌクレオシドの合成研究
- DNAの損傷と修復の生物有機化学的研究
- チオ糖誘導体の合成と生物活性
- ヌクレオシド系抗生物質の全合成研究
- ヌクレオシド系代拮抗剤の開発研究
- Bio-organic Chemistry for DNA damage and repair
- Chemical Synthesis and Biological Activity of Thio Sugar Derivatives
- Total Synthesis of Nucleoside Antibiotic
- Development of New Synthetic Method for Biologically Active Nucleoside Derivatives
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Papers (47):
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Kazuhiro Haraguchi, Hiroki Kumamoto, Shuhei Imoto, Nobuyo Kuwata-Higashi, Hiroaki Mitsuya. Regio- and Stereoselective Synthesis of 2′-Deoxy-4′-thioguanine Nucleosides: Evaluation of Anti-Hepatitis B Virus Activity and Cytotoxicity Leading to Improved Selectivity Index by 4′-C-Cyanation. Synlett. 2023. 35. 06. 728-733
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Hiroki Kumamoto, Nobuyo Higashi-Kuwata, Sanae Hayashi, Debananda Das, Haydar Bulut, Ryoh Tokuda, Shuhei Imoto, Kengo Onitsuka, Yuka Honda, Yuki Odanaka, et al. Synthesis of novel entecavir analogues having 4'-cyano-6''-fluoromethylenecyclopentene skeletons as an aglycone moiety as highly potent and long-acting anti-hepatitis B virus agent. RSC advances. 2023. 13. 23. 15999-16011
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Hiroki Kumamoto, Nobuyo Higashi-Kuwata, Sanae Hayashi, Debananda Das, Haydar Bulut, Ryoh Tokuda, Shuhei Imoto, Kengo Onitsuka, Yuka Honda, Yuki Odanaka, et al. Synthesis of novel entecavir analogues having 4′-cyano-6′′-fluoromethylenecyclopentene skeletons as an aglycone moiety as highly potent and long-acting anti-hepatitis B virus agent. RSC Advances. 2023. 13. 23. 15999-16011
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Kazuhiro Haraguchi, Hiroki Kumamoto, Hiromichi Tanaka. 4-Thiofuranoid Glycal: Versatile Glycosyl Donor for the Selective Synthesis of β-anomer of 4'-thionucleoside and its Biological Activities. Current medicinal chemistry. 2022. 29. 21. 3684-3731
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Kazuhiro Haraguchi, Eisen Gen, Hiroki Kumamoto, Yoshiharu Itoh, Hiromichi Tanaka. An alternative method for the synthesis of 2'-halogeno-1',2'-unsaturated uridine derivatives through syn-elimination of pivalic acid of 2'-halogeno- 2'-deoxy-1'-pivaloyloxyuracil nucleoside: preparation of its 2'-C-branched nucleosides. Nucleosides, nucleotides & nucleic acids. 2020. 39. 1-3. 426-438
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MISC (177):
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From synthetic chemistry of nucleosides to new antiviral agents. The Showa University journal of pharmaceutical sciences. 2010. 1. 2. 109-125
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紺野奇重, 原口一広, 田中博道. m-CPBAによるエリスロフラノイドグリカールのタンデム型エポキシ化/m-クロロベンゾイルオキシ化反応:psicofuranose誘導体の新規合成法の開発と糖供与体としての利用. 日本薬学会年会要旨集. 2010. 130th. 2
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Hiroki Kumamoto, Kazuhiro Haraguchi, Mayumi Ida, Kazuo T. Nakamura, Yasuyuki Kitagawa, Takayuki Hamasaki, Masanori Baba, Satoko Shimbara Matsubayashi, Hiromichi Tanaka. Synthesis of (+/-)-4 '-ethynyl-5 ',5 '-difluoro-2 ',3 '-dehydro-3 '-deoxy- carbocyclic thymidine: a difluoromethylidene analogue of promising anti-HIV agent Ed4T. TETRAHEDRON. 2009. 65. 36. 7630-7636
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Hisashi Shimada, Satoshi Kikuchi, Saori Okuda, Kazuhiro Haraguchi, Hiromichi Tanaka. Nucleophilic substitution approach to 4 '-substituted thymidines by employing 4 '-benzenesulfonyl leaving group. TETRAHEDRON. 2009. 65. 31. 6008-6016
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Yutaka Kubota, Mayumi Kunikata, Kazuhiro Haraguchi, Hiromichi Tanaka. Solvent Effect Observed in Nucleophilic Substitution of 4 '-(Benzoyloxy)cordycepin with AlMe3: Stereochemical Evidence for S(N)i Mechanism. JOURNAL OF ORGANIC CHEMISTRY. 2009. 74. 9. 3402-3405
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Patents (2):
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1'位炭素置換ピリミジンヌクレオシドおよびその製造法
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4'-炭素置換ピリミジンヌクレオシド及びその製造法
Books (4):
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新編 医薬化学
廣川書店 2018
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Next Generation Anti-HIV Agent 4’-Ethynylstavudine: From The Bench To The Clinic
2015
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"HEPT : From an Investigation of Lithiation of Nucleoside Towards a Rational Design of Non-nucleosides Reverse Transcriptase Inhibitors of HIV-1
Advance in Antiviral Drug Design JAI Press 1999
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"HEPT : From an Investigation of Lithiation of Nucleoside Towards a Rational Design of Non-nucleosides Reverse Transcriptase Inhibitors of HIV-1
Advance in Antiviral Drug Design JAI Press 1999
Lectures and oral presentations (10):
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m-CPBAによるエリスロフラノイドグリカールのタンデム型エポキシ化/m-クロロベンゾイルオキシ化反応:psicofuranose誘導体の新規合成法の開発と糖供与体としての利用
(日本薬学会第130年会 2010)
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糖部4’位に置換基を有するヌクレオシドホスホネート誘導体の合成とその抗ウイルス活性
(日本薬学会第130年会 2010)
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エポキシ糖の反応性を利用する立体制御された分岐糖ヌクレオシドの合成法の確立:抗HIV活性を有するFestinavirの開発
(日本薬学会第130年会 2010)
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フラノイドグリカールを利用する面選択的なグリコシル化反応:アノマー位が分岐したチミジン誘導体の合成研究
(日本薬学会129年会 2009)
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糖部4’位のベンゼンスルフェニル化を鍵反応とする4’-置換コルジセピンンの新規合成法の開発
(日本薬学会129年会 2009)
more...
Works (3):
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抗HIV作用を有する化合物の創製
2002 -
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1'-炭素鎖置換プリンヌクレオシド及びその製造法
1995 -
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Synthetic Method for the Preparation of 1'-C-Branched Pyrimidine Nucleosides
1993 -
Education (4):
- - 1988 Showa University Pharmaceutical Scientific Research Division
- - 1988 Showa University Graduate School, School of Pharmaceutical Sciences
- - 1983 Showa University School of Pharmacy Division of Pharmacology
- - 1983 Showa University Faculty of Pharmaceutical Science School of Pharmaclutical Sciences
Professional career (1):
- (BLANK) (Showa University)
Work history (7):
- 2013/04 - 2018/09 Nihon Pharmaceutical University Nihon Pharmaceutical University
- 2004/04 - 2013/03 Showa University School of Pharmacy
- 1998 - 2003 Showa University School of Pharmacy
- 1998 - 2003 Associate Professor, School of Pharmaceutical
- 1988 - 1998 Showa University School of Pharmacy
- 1988 - 1998 Research Associate, School of Pharmaceutical
- Sciences, Showa University
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Awards (8):
- 2010 - The Pharmaceutical Society of Japan, Sato Memorial Award
- 2003 - 薬学研究奨励財団 奨励賞
- 2003 - The Research Foundation for Pharmaceutical Sciences Promoted Research Award
- 2002 - ポスター賞
- 2002 - Poster Award
- 1992 - 上原記念生命科学財団奨励賞
- 1992 - Uehara Memorial Foundation, Promoted Research Award
- 平成22年日本薬学会佐藤記念賞
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Association Membership(s) (3):
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