Výsledky vyhledávání - "Tomoyuki Odani"

Discovery of a novel series of indolinylpyrimidine-based GPR119 agonists: Elimination of ether-a-go-go-related gene liability using a hydrogen bond acceptor-focused approach

Autor: Yoshiyuki Tsujihata, Hirohisa Miyashita, Kae Matsuda, Masahiro Kamaura, Shin-ichi Abe, Kenjiro Sato, Tomoyuki Odani, Osamu Kubo, Hiromichi Sugimoto, Toshiki Murata, Shinji Iwasaki, Naoyoshi Noguchi

Publikováno v: Bioorganicmedicinal chemistry. 34

We previously identified a novel series of indolinylpyrimidine derivatives exemplified by 2 in Figure 1, which is an indoline based derivative, as potent GPR119 agonists. Despite the attractive potency of 2, this compound inhibited the human ether-a-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::166ee25c74829d63bf2f8da183f611d5
https://pubmed.ncbi.nlm.nih.gov/33548803

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Discovery of a novel series of GPR119 agonists: Design, synthesis, and biological evaluation of N-(Piperidin-4-yl)-N-(trifluoromethyl)pyrimidin-4-amine derivatives

Autor: Tomoyuki Kitazaki, Kae Matsuda, Hirohisa Miyashita, Shinji Iwasaki, Kenjiro Sato, Shin-ichi Abe, Masahiro Kamaura, Koji Watanabe, Toshiki Murata, Kazuaki Takami, Osamu Kubo, Tomoyuki Odani, Yoshiyuki Tsujihata

Publikováno v: Bioorganic & Medicinal Chemistry. 41:116208

We undertook an optimization effort involving propan-2-yl 4-({6-[5-(methanesulfonyl)-2,3-dihydro-1H-indol-1-yl]pyrimidin-4-yl}oxy)piperidine-1-carboxylate 1, which we had previously discovered as a novel G protein-coupled receptor 119 (GPR119) agonis

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::06da7da98d8f5f5b1b8d577e5040d395
https://doi.org/10.1016/j.bmc.2021.116208

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Discovery of novel somatostatin receptor subtype 5 (SSTR5) antagonists: Pharmacological studies and design to improve pharmacokinetic profiles and human Ether-a-go-go-related gene (hERG) inhibition

Autor: Yoshihide Nakano, Tsuyoshi Maekawa, Takashi Nakahata, Masanori Watanabe, Shinji Iwasaki, Sachie Morimoto, Asato Kina, Shizuo Kasai, Nobuyuki Takakura, Takeshi Yamasaki, Yuji Shimizu, Yumiko Okano Tamura, Tohru Yamashita, Tomoyuki Odani, Jun Sugama, Hideki Hirose

Publikováno v: Bioorganic & Medicinal Chemistry. 25:4153-4162

Somatostatin (SST) is a peptide hormone comprising 14 or 28 amino acids that inhibits endocrine and exocrine secretion via five distinct G-protein-coupled receptors (SSTR1-5). SSTR5 has an important role in inhibiting the secretion of pancreatic and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e7e142ba64317c5da625db4c39b32b21
https://doi.org/10.1016/j.bmc.2017.06.003

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Identification and Characterization of a New Series of Ghrelin O-Acyl Transferase Inhibitors

Autor: Mariko Yoneyama-Hirozane, Shiro Takekawa, Junichi Sakamoto, Kenichi Imahashi, Tsuyoshi Ishii, Junji Matsui, Yoshihide Nakano, Takeshi Hirakawa, Kohei Deguchi, Tomoyuki Odani, Ikumi Chisaki, Nobuyuki Takakura

Publikováno v: SLAS discovery : advancing life sciences RD. 23(2)

Ghrelin O-acyl transferase (GOAT; MBOAT4) catalyzes O-acylation at serine-3 of des-acyl ghrelin. Acyl ghrelin is secreted by stomach X/A-like cells and plays a role in appetite and metabolism. Therefore, GOAT has been expected to be a novel antiobesi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4881be1b8d192e44fa7e4e2ebdc29007
https://pubmed.ncbi.nlm.nih.gov/28846466

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Discovery of the First Potent and Orally Available Agonist of the Orphan G-Protein-Coupled Receptor 52

Autor: Eri Shiraishi, Tomoyuki Odani, Teruki Hamada, Masakuni Kori, Hiroyuki Ota, Masaki Setoh, Miyanohana Yuhei, Naoyuki Kanzaki, Kazunobu Aoyama, Naoki Ishii, Toshiya Harasawa, Mitsunori Kono

Publikováno v: Journal of Medicinal Chemistry. 57:5226-5237

G-protein-coupled receptor 52 (GPR52) is an orphan Gs-coupled G-protein-coupled receptor. GPR52 inhibits dopamine D2 receptor signaling and activates dopamine D1/N-methyl-d-aspartate receptors via intracellular cAMP accumulation, and therefore, GPR52

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e50db0b0f93bb3dc09acf9673ebd7a82
https://doi.org/10.1021/jm5002919

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Discovery of a novel series of indoline carbamate and indolinylpyrimidine derivatives as potent GPR119 agonists

Autor: Kentaro Rikimaru, Kenjiro Sato, Hirohisa Miyashita, Toshiki Murata, Tomoyuki Odani, Yoshiyuki Tsujihata, Hiroshi Imoto, Hiromichi Sugimoto, Nobuyuki Negoro, Masahiro Kamaura

Publikováno v: Bioorganic & Medicinal Chemistry. 22:1649-1666

GPR119 has emerged as an attractive target for anti-diabetic agents. We identified a structurally novel GPR119 agonist 22c that carries a 5-(methylsulfonyl)indoline motif as an early lead compound. To generate more potent compounds of this series, st

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2562b7ee232d9914f1ede62296113b39
https://doi.org/10.1016/j.bmc.2014.01.028

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Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist

Publikováno v: ACS Medicinal Chemistry Letters. 1:290-294

GPR40, one of the G protein-coupled receptors predominantly expressed in pancreatic β-cells, mediates enhancement of glucose-stimulated insulin secretion by free fatty acids. A potent and selective GPR40 agonist is theorized to be a safe and effecti

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::474754ccb19926b60115c8dfbd7acc08
https://doi.org/10.1021/ml1000855

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Reduced bactericidal activity and nitric oxide production in metallothionein-deficient macrophages in response to lipopolysaccharide stimulation

Autor: Tsuyoshi Nakanishi, Tomoyuki Odani, Norio Itoh, Masako Kanekiyo, Keiichi Tanaka, Dunkokkuruad Namphung, Akiko Matsuyama, Hiroshi Shibayama

Publikováno v: Toxicology. 216:188-196

This study was designed to investigate bactericidal activity of and nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated peritoneal exudate macrophages (Mvarphi) from metallothionein (MT)-null mice. Control Mvarphi had a bactericidal e

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d33a74c2ad994ac59a4f2d46e463a52a
https://doi.org/10.1016/j.tox.2005.08.005

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Detection of increased icb-1 transcript levels in maturing HL-60 cells: a novel marker for granulocytic and monocytic in vitro differentiation

Autor: Keiichi Tanaka, O. Ortmann, Klaus Diedrich, Norio Itoh, Jyunya Kohroki, Tsuyoshi Nakanishi, Harue Imai, O. Treeck, Sayaka Fujita, Tomoyuki Odani, Günter Vollmer

Publikováno v: Leukemia Research. 26:765-769

Human gene icb-1 was initially described as a gene with increased expression in endometrial tumor cells differentiated in vitro by culture on a reconstituted basement membrane. We provide evidence for a more general involvement of icb-1 gene function

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ae28882bb49ca935434a5a02ce290b15
https://doi.org/10.1016/s0145-2126(02)00005-x

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Design, synthesis, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase inhibitors

Autor: Takahiro Matsumoto, Yohei Kosugi, Toru Kawamura, Mitsunori Kono, Tomoyuki Odani, Shinji Fujimoto, Hideki Matsui, Toshihiro Imaeda, Yuji Shimizu, Masakuni Kori, Masato Shimojo

Publikováno v: Bioorganicmedicinal chemistry. 22(4)

A series of piperazine ureas were designed, synthesized, and evaluated for their potential as novel orally efficacious fatty acid amide hydrolase (FAAH) inhibitors for the treatment of neuropathic and inflammatory pain. We carried out an optimization

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2b9981d56044efceb833957d2c4f1243
https://pubmed.ncbi.nlm.nih.gov/24440478

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