Výsledky vyhledávání - "Eiji, Kawanishi"

Synthesis and properties of GuNA purine/pyrimidine nucleosides and oligonucleotides

Autor: Tomo Takegawa-Araki, Eiji Kawanishi, Shinji Kumagai, Katsuya Yamada, Naohiro Horie, Hiroaki Sawamoto, Takao Yamaguchi, Yuuki Arai, Tetsuya Ohta, Shuhei Yamakoshi, Satoshi Obika

Publikováno v: Organic & Biomolecular Chemistry. 18:9461-9472

We recently designed guanidine-bridged nucleic acids (GuNA), and GuNA bearing a thymine (T) nucleobase was synthesized and successfully incorporated into oligonucleotides. The GuNA-T-modified oligonucleotides possessed high duplex-forming ability tow

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f09667d5e31414d8a80ac54f9f5ad471
https://doi.org/10.1039/d0ob01970d

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Selective covalent targeting of SARS-CoV-2 main protease by enantiopure chlorofluoroacetamide

Autor: Rui Hamada, Kenji Mizuguchi, Tadanari Hiramoto, Akio Ojida, Suyong Re, Hikaru Isogai, Daiki Yamane, Satsuki Onitsuka, Naoya Shindo, Eiji Kawanishi

Publikováno v: Chemical science. 13(10)

The pandemic of COVID-2019 has urged the development of antiviral agents against its causative pathogen SARS-CoV-2. The main protease (Mpro), a cysteine protease essential for viral replication, is a promising protein target. Here we report an irreve

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::54ff954ac39de22964e4fe2745ba627c
https://pubmed.ncbi.nlm.nih.gov/35432850

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Scalable Process Design for a PDE10A Inhibitor Consisting of Pyrazolopyrimidine and Quinoxaline as Key Units

Autor: Masuhiro Sugino, Takehiro Nanjo, Ryo Kobayashi, Eiji Toyofuku, Shinichi Izumoto, Noriaki Moriyama, Masayuki Utsugi, Takafumi Yamagami, Yoichi Kadoh, Hajime Hiramatsu, Hideki Horiuchi, Yasunori Moritani, Eiji Kawanishi

Publikováno v: Organic Process Research & Development. 23:578-587

In this study, research and development for the synthetic process of a PDE10A inhibitor are described; in particular, an efficient regioselective construction of the quinoxaline unit, a cost-effective pyrazolo[1,5-a]pyrimidine formation, and a cost-s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ec51d299ba796e24997f1576adcc473e
https://doi.org/10.1021/acs.oprd.9b00068

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Discovery of 2-[(E)-2-(7-Fluoro-3-methylquinoxalin-2-yl)vinyl]-6-pyrrolidin-1-yl-N-(tetrahydro-2H-pyran-4-yl)pyrimidin-4-amine Hydrochloride as a Highly Selective PDE10A Inhibitor

Autor: Kei Takedomi, Eiji Kawanishi, Yumi Watanabe, Mayumi Kimura, Koki Kojima, Yoichi Kadoh, Yoshihito Tanaka, Takehiko Matsumura, Kenji Omori, Tamaki Kobayashi, Toshiaki Sakamoto, Haruko Miyoshi, Jun Kotera, Toshiyuki Himiyama, Mitsuya Hongu, Takashi Sasaki, Hiroyuki Taniguchi

Publikováno v: Chemical and Pharmaceutical Bulletin. 66:243-250

Phosphodiesterase (PDE) 10A is a dual hydrolase of cAMP and cGMP and highly expressed in striatal medium spiny neurons. Inhibition of PDE10A modulates the activity of medium spiny neurons (MSN) via the regulation of cAMP and cGMP. Signal control of M

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e6843e881235274aefe3a3c26a35ba5a
https://doi.org/10.1248/cpb.c17-00783

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Discovery of a pyrazolo[1,5-a]pyrimidine derivative (MT-3014) as a highly selective PDE10A inhibitor via core structure transformation from the stilbene moiety

Autor: Takehiko Matsumura, Hiroyuki Taniguchi, Takashi Sasaki, Misae Takakuwa, Haruko Miyoshi, Yoichi Kadoh, Eiji Kawanishi, Mitsuya Hongu, Yoshihito Tanaka, Yumi Watanabe, Kei Takedomi, Nobuyuki Baba, Yuuki Koizumi, Jun Kotera, Koki Kojima, Itsuko Nakamura

Publikováno v: Bioorganicmedicinal chemistry. 27(15)

We have developed a new class of PDE10A inhibitor, a pyrazolo[1,5-a]pyrimidine derivative MT-3014 (1). A previous compound introduced was deprioritized due to concerns for E/Z-isomerization and glutathione-adduct formation at the core stilbene struct

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4bd08f7ec18e9eee0e29fcebbf425ca7
https://pubmed.ncbi.nlm.nih.gov/31235264

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Synthetic Method for 2'-Amino-LNA Bearing Any of the Four Nucleobases via a Transglycosylation Reaction

Autor: Shuhei Yamakoshi, Satoshi Obika, Eiji Kawanishi, Yuuki Arai, Hiroaki Sawamoto

Publikováno v: Organic letters. 20(7)

A transglycosylation reaction of 2′-amino-locked nucleic acid (LNA) from thymine (T) to other nucleobases adenine (A), guanine (G), and 5-methylcytosine (mC) has been developed. This reaction proceeds in high yield and with high β-selectivity. The

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c0a96a4d4d8b012b4cecda21a9b3b342
https://pubmed.ncbi.nlm.nih.gov/29528240

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