Výsledky vyhledávání - "NORIKAZU OHTAKE"

Lead Identification of 8-(Methylamino)-2-oxo-1,2-dihydroquinoline Derivatives as DNA Gyrase Inhibitors: Hit-to-Lead Generation Involving Thermodynamic Evaluation

Autor: Aiko Masuko, Hiroyuki Sugiyama, Fumihito Ushiyama, Harumi Kanazawa, Koichiro Nakano, Norikazu Ohtake, Masashi Mima, Kosuke Hitaka, Hideaki Amada, Takeuchi Tomoki, Nozomi Tanaka-Yamamoto, Kunihiko Iwamoto, Iichiro Takata

Publikováno v: ACS Omega
ACS Omega, Vol 5, Iss 17, Pp 10145-10159 (2020)

DNA gyrase and topoisomerase IV are well-validated pharmacological targets, and quinolone antibacterial drugs are marketed as their representative inhibitors. However, in recent years, resistance to these existing drugs has become a problem, and new

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b7ab8f6fd6bd3f2be8c5a152b9adb049
https://doi.org/10.1021/acsomega.0c00865

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Lead optimization of 8-(methylamino)-2-oxo-1,2-dihydroquinolines as bacterial type II topoisomerase inhibitors

Autor: Mayumi Endo, Hideaki Amada, Masafumi Kamitani, Takeuchi Tomoki, Norikazu Ohtake, Yunoshin Tamura, Aiko Masuko, Nozomi Tanaka-Yamamoto, Hiroyuki Sugiyama, Fumihito Ushiyama, Yasuhiro Mihara, Kosuke Hitaka, Iichiro Takata, Reiko Wada, Masashi Mima

Publikováno v: Bioorganicmedicinal chemistry. 28(22)

The global increase in multidrug-resistant pathogens has caused severe problems in the treatment of infections. To overcome these difficulties, the advent of a new chemical class of antibacterial drug is eagerly desired. We aimed at creating novel an

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c778902e9c7dd887132f2d7e97ce1d0
https://pubmed.ncbi.nlm.nih.gov/33032189

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Discovery of MGS0274, an ester prodrug of a metabotropic glutamate receptor 2/3 agonist with improved oral bioavailability

Autor: Naoki Miyakoshi, Motoki Ochi, Toshiyuki Marumo, Misako Fukasawa, Takashi Hashihayata, Hiroki Urabe, Akiko Nozoe, Junichi Yamaguchi, Kohnosuke Kinoshita, Shigeyuki Chaki, Norikazu Ohtake, Hirohiko Hikichi

Publikováno v: European journal of medicinal chemistry. 203

We previously reported that MGS0008 is a selective group II metabotropic glutamate receptor (mGlu2/3 receptor) agonist that is effective in animal models of schizophrenia. MGS0008 is a highly hydrophilic glutamate analog and is therefore expected to

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4dd7fdcf1e674d170275b8838d244759
https://pubmed.ncbi.nlm.nih.gov/32698110

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Design, synthesis and biological evaluation of novel 7-azaspiro[3.5]nonane derivatives as GPR119 agonists

Autor: Norikazu Ohtake, Keiko Fusegi, Fumiyasu Shiozawa, Masako Miyoshi, Madoka Kawamura, Matsuda Daisuke, Kayo Kimura, Hiroyuki Kakinuma, Youichirou Suga, Noriko Takayama, Shinichi Nishimoto, Yohei Kobashi

Publikováno v: Bioorganic & Medicinal Chemistry. 26:1832-1847

The design and synthesis of a novel class of 7-azaspiro[3.5]nonane GPR119 agonists are described. In this series, optimization of the right piperidine N-capping group (R2) and the left aryl group (R3) led to the identification of compound 54g as a po

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::40f6884b547f8c83165973717d1c2040
https://doi.org/10.1016/j.bmc.2018.02.032

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Identification of highly selective and potent orexin receptor 1 antagonists derived from a dual orexin receptor 1/2 antagonist based on the structural framework of pyrazoylethylbenzamide

Autor: Futamura Aya, Dai Nozawa, Seiken Tokura, Yuichi Tokumaru, Yuko Araki, Norikazu Ohtake, Yunoshin Tamura, Hiroshi Kawamoto, Sora Kakihara, Takeshi Aoki

Publikováno v: Bioorganic & Medicinal Chemistry. 25:5203-5215

The design, synthesis, and structure activity relationships of the novel class of pyrazolylethylbenzamide orexin receptor 1-selective antagonists are described. Further derivatization of the prototype dual orexin receptor 1/2 antagonist lead (1) by i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::08f07cf6376c75baf1059cdd28966fe0
https://doi.org/10.1016/j.bmc.2017.07.051

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High-Contrast PET Imaging of Vasopressin V1B Receptors with a Novel Radioligand, 11C-TASP699

Autor: Satoshi Ozaki, Norikazu Ohtake, Makoto Higuchi, Masayuki Hanyu, Yuji Nagai, Tetsuya Suhara, Ming-Rong Zhang, Kazumi Koga, Shigeyuki Chaki, Mitsukane Yoshinaga

Publikováno v: Journal of Nuclear Medicine. 58:1652-1658

Vasopressin 1B receptors (V1BRs) are abundantly expressed in the pituitary, and in vivo PET of V1BRs was recently enabled by our development of a specific radioligand, 11C-TASP0434299, derivatized from pyridopyrimidin-4-one. Here, we identified a nov

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8f4cb500f0fa672f27dad8d9b891ae67
https://doi.org/10.2967/jnumed.116.188698

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Design and synthesis of 1H-pyrazolo[3,4-c]pyridine derivatives as a novel structural class of potent GPR119 agonists

Autor: Madoka Kawamura, Masako Miyoshi, Fumiyasu Shiozawa, Yohei Kobashi, Kayo Kimura, Shinichi Nishimoto, Hiroyuki Kakinuma, Kenichi Kawabe, Matsuda Daisuke, Ayako Mikami, Koji Oda, Noriko Takayama, Makoto Hamada, Norikazu Ohtake

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 26:3441-3446

Design and synthesis of a novel class of 1H-pyrazolo[3,4-c]pyridine GPR119 receptor agonists are described. Lead compound 4 was identified through the ligand-based drug design approach. Modification of the left-hand aryl group (R(1)) and right-hand p

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0622782d072387d87dd6a5a5b735a492
https://doi.org/10.1016/j.bmcl.2016.06.050

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