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837 results on '"Hosoya, Takamitsu"'

1. Monte Carlo simulation of molecular dynamics for amino acid production from carboxylic acid via C-14 beta-decay

Author

Fukuchi, Tomonori, Niwa, Takashi, Hosoya, Takamitsu, and Watanabe, Yasuyoshi

Subjects
Physics - Chemical Physics, Physics - Computational Physics
Abstract

To study the chemical origin of life, we investigated the amino acid production probability from radiocarbon (C-14)-containing carboxylic acid via beta-decay using a newly developed Monte Carlo simulator for molecular dynamics calculation. Using the simulation, we calculated the dynamical trajectory of N-14 recoiled via C-14 beta-decay in [3-C-14]propionic acid and evaluated the staying probability of N-14 in the compound, which is the glycinium (a protonated glycine) production probability from [3-C-14]propionic acid. The glycinium production probability was calculated to be 78.7% assuming static compound structures of [3-C-14]propionic acid and a glycinium C-N binding potential energy of 3.93 eV. From calculations with various binding potential parameters, a glycinium production probability of approximately 30% was expected by simulation in case of a loose C-N binding potential energy of 2-eV., Comment: 11 pages, 6 figures, submitted to PLOS ONE Journal

Published
2021
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5. Clinical evaluation of [18F]pitavastatin for quantitative analysis of hepatobiliary transporter activity

Author

Nakaoka, Takayoshi, Kaneko, Ken-ichi, Irie, Satsuki, Mawatari, Aya, Igesaka, Ami, Uetake, Yuta, Ochiai, Hidenori, Niwa, Takashi, Yamano, Emi, Wada, Yasuhiro, Tanaka, Masaaki, Kotani, Kohei, Kawahata, Hideki, Kawabe, Joji, Miki, Yukio, Doi, Hisashi, Hosoya, Takamitsu, Kazuya, Maeda, Kusuhara, Hiroyuki, Sugiyama, Yuichi, and Watanabe, Yasuyoshi

Published
2022
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16. Comparison of pharmacokinetics of newly discovered aromatase inhibitors by a cassette microdosing approach in healthy Japanese subjects

Author

Kusuhara, Hiroyuki, Takashima, Tadayuki, Fujii, Hisako, Takashima, Tsutomu, Tanaka, Masaaki, Ishii, Akira, Tazawa, Shusaku, Takahashi, Kazuhiro, Takahashi, Kayo, Tokai, Hidekichi, Yano, Tsuneo, Kataoka, Makoto, Inano, Akihiro, Yoshida, Suguru, Hosoya, Takamitsu, Sugiyama, Yuichi, Yamashita, Shinji, Hojo, Taisuke, and Watanabe, Yasuyoshi

Published
2017
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20. Synthesis of 11C-Radiolabeled Eribulin as a Companion Diagnostics PET Tracer for Brain Glioblastoma

Author

Niwa, Takashi, primary, Tahara, Tsuyoshi, additional, Chase, Charles E., additional, Fang, Francis G., additional, Nakaoka, Takayoshi, additional, Irie, Satsuki, additional, Hayashinaka, Emi, additional, Wada, Yasuhiro, additional, Mukai, Hidefumi, additional, Masutomi, Kenkichi, additional, Watanabe, Yasuyoshi, additional, Cui, Yilong, additional, and Hosoya, Takamitsu, additional

Published
2023
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30. 11C‐Cyanation of Aryl Fluorides via Nickel and Lithium Chloride‐Mediated C−F Bond Activation.

Author

Zhang, Zhouen, Niwa, Takashi, Watanabe, Kenji, and Hosoya, Takamitsu

Subjects
NICKEL, FLUORIDES, OXIDATIVE addition, CHEMICAL precursors, CHEMICAL stability, SCISSION (Chemistry), ARYL chlorides, CHLORIDE channels
Abstract

Aryl fluorides are expected to be useful as radiolabeling precursors due to their chemical stability and ready availability. However, direct radiolabeling via carbon‐fluorine (C−F) bond cleavage is a challenging issue due to its significant inertness. Herein, we report a two‐phase radiosynthetic method for the ipso‐11C‐cyanation of aryl fluorides to obtain [11C]aryl nitriles via nickel‐mediated C−F bond activation. We also established a practical protocol that avoids the use of a glovebox, except for the initial preparation of a nickel/phosphine mixture, rendering the method applicable for general PET centers. This method enabled the efficient synthesis of diverse [11C]aryl nitriles from the corresponding aryl fluorides, including pharmaceutical drugs. Stoichiometric reactions and theoretical studies indicated a significant promotion effect of lithium chloride on the oxidative addition, affording an aryl(chloro)nickel(II) complex, which serves as a precursor for rapid 11C‐cyanation. [ABSTRACT FROM AUTHOR]

Published
2023
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45. CDK9 inhibitor FIT-039 prevents replication of multiple DNA viruses

Author

Yamamoto, Makoto, Onogi, Hiroshi, Kii, Isao, Yoshida, Suguru, Iida, Kei, Sakai, Hiroyuki, Abe, Minako, Tsubota, Toshiaki, Ito, Nobutoshi, and Hosoya, Takamitsu

Subjects
DNA viruses -- Research -- Health aspects, Protein kinases -- Physiological aspects -- Research, Health care industry
Abstract

A wide range of antiviral drugs is currently available; however, drug-resistant viruses have begun to emerge and represent a potential public health risk. Here, we explored the use of compounds that inhibit or interfere with the action of essential host factors to prevent virus replication. In particular, we focused on the cyclin-dependent kinase 9 (CDK9) inhibitor, FIT-039, which suppressed replication of a broad spectrum of DNA viruses through inhibition of mRNA transcription. Specifically, FIT-039 inhibited replication of herpes simplex virus 1 (HSV-1), HSV-2, human adenovirus, and human cytomegalovirus in cultured cells, and topical application of FIT-039 ointment suppressed skin legion formation in a murine HSV-1 infection model. FIT-039 did not affect cell cycle progression or cellular proliferation in host cells. Compared with the general CDK inhibitor flavopiridol, transcriptome analyses of FIT-039-treated cells revealed that FIT-039 specifically inhibited CDK9. Given at concentrations above the inhibitory concentration, FIT-039 did not have a cytotoxic effect on mammalian cells. Importantly, administration of FIT-039 ameliorated the severity of skin lesion formation in mice infected with an acyclovir-resistant HSV-1, without noticeable adverse effects. Together, these data indicate that FIT-039 has potential as an antiviral agent for clinical therapeutics., Introduction The number of available antiviral drugs has increased continually since the development of azidothymidine and acyclovir (ACV) in the 1970s (1,2). However, this has resulted in the emergence of [...]

Published
2014
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46. Synthesis of Multisubstituted Benzenes from Phenols via Multisubstituted Benzynes.

Author

Nagai, Akira, Kobayashi, Akihiro, Sakata, Yuki, Minami, Yasunori, Uchida, Keisuke, Hosoya, Takamitsu, and Yoshida, Suguru

Subjects
BENZYNES, BENZENE synthesis, PHENOL, AROMATIC compounds, ARYNE
Abstract

A new method to synthesize multifunctionalized arenes from simple phenols through aryne intermediates is described. Multisubstituted aryne precursors were prepared from phenols by Ir-catalyzed C–H borylation, deborylthiolation, O -triflylation, S -oxidation, and further modification through ortho -deprotonation directed by the sulfoxide moiety. Various multisubstituted arenes were synthesized by transformations of highly functionalized aryne intermediates generated from the o -sulfinylaryl triflates. [ABSTRACT FROM AUTHOR]

Published
2022
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