Literature DB >> 18226899

Radiosyntheses of two positron emission tomography probes: [11C]Oseltamivir and its active metabolite [11C]Ro 64-0802.

Fujiko Konno1, Takuya Arai, Ming-Rong Zhang, Akiko Hatori, Kazuhiko Yanamoto, Masanao Ogawa, Gukuto Ito, Chika Odawara, Tomoteru Yamasaki, Koichi Kato, Kazutoshi Suzuki.   

Abstract

Oseltamivir phosphate (Tamiflu, 1.H(3)PO(4) is an orally active anti-influenza drug, which is hydrolyzed by esterase to its carboxylate metabolite Ro 64-0802 (2) with potent activity inhibiting neuraminidase. In this study, for the first time, we synthesized carbon-11-labeled oseltamivir ([(11)C]1) and Ro 64-0802 ([(11)C]2) as two novel positron emission tomography probes and demonstrated that [(11)C]1 had twofold higher radioactivity concentration in the mouse brains than [(11)C]2.

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Year:  2008        PMID: 18226899     DOI: 10.1016/j.bmcl.2008.01.037

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Enantioselective Synthesis of Oseltamivir Phosphate (Tamiflu) via the Iron-Catalyzed Stereoselective Olefin Diazidation.

Authors:  Hongze Li; Shou-Jie Shen; Cheng-Liang Zhu; Hao Xu
Journal:  J Am Chem Soc       Date:  2018-08-09       Impact factor: 15.419

Review 2.  Radiolabeled antiviral drugs and antibodies as virus-specific imaging probes.

Authors:  Mike Bray; Michele Di Mascio; Fabian de Kok-Mercado; Daniel J Mollura; Elaine Jagoda
Journal:  Antiviral Res       Date:  2010-08-13       Impact factor: 5.970

  2 in total

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