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

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Papers (43)：

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
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
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
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
Shuhei Imoto, Kengo Onitsuka, Kakeru Yamaguchi, Ryoh Tokuda, Nobuyo Higashi-Kuwata, Shunsuke Kuwahara, Hiroki Kumamoto, Kenji Maeda, Kazuhiro Haraguchi, Hiroaki Mitsuya. Design and Synthesis of 4'-Cyano Dideoxy Isonucleosides and Their Activity against HIV-1 and HBV. HETEROCYCLES. 2020. 100. 10. 1599-1599

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MISC (177)：

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Patents (2)：

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
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)：

新編医薬化学
廣川書店 2018
Next Generation Anti-HIV Agent 4’-Ethynylstavudine: From The Bench To The Clinic
2015
"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
"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)：

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)
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)
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)
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)
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)

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Works (3)：

抗HIV作用を有する化合物の創製
2002 -
1'-炭素鎖置換プリンヌクレオシド及びその製造法
1995 -
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

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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

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Association Membership(s) (3)：

有機合成化学協会 , 日本化学会 , 日本薬学会

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