Výsledky vyhledávání - "Madoka Kawamura"

Discovery of Novel Pyrazolylpyridine Derivatives for 20-Hydroxyeicosatetraenoic Acid Synthase Inhibitors with Selective CYP4A11/4F2 Inhibition

Autor: Madoka Kawamura, Yohei Kobashi, Hiroaki Tanaka, Ayako Bohno-Mikami, Makoto Hamada, Yuji Ito, Takashi Hirata, Hiroki Ohara, Naoki Kojima, Hiroko Koretsune, Emi Gunji, Takuya Fukunaga, Shoko Inatani, Yoshitaka Hasegawa, Akinori Suzuki, Teisuke Takahashi, Hiroyuki Kakinuma

Publikováno v: Journal of Medicinal Chemistry. 65:14599-14613

20-Hydroxyeicosatetraenoic acid (20-HETE) is one of the major oxidized arachidonic acid (AA) metabolites produced by cytochrome P450 (CYP) 4A11 and CYP4F2 isozymes in the human liver and kidney. Numerous studies have suggested the involvement of 20-H

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5d86e880078af477f959a903c5a9ea20
https://doi.org/10.1021/acs.jmedchem.2c01089

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Synthesis and Structure-Activity Relationship of C-Phenyl D-Glucitol (TP0454614) Derivatives as Selective Sodium-Dependent Glucose Cotransporter 1 (SGLT1) Inhibitors

Autor: Hiroyuki Kakinuma, Yuki Shimizu, Kayo Kimura, Yohei Kobashi, Lisa Okumura-Kitajima, Makoto Hamada, Koji Yamamoto, Hiroko Koretsune, Kuroda Shoichi, Kenichi Kawabe, Fumiyasu Shiozawa, Madoka Kawamura

Publikováno v: Chemicalpharmaceutical bulletin. 68(7)

Sodium-glucose cotransporter 1 (SGLT1) is the primary transporter for glucose absorption from the gastrointestinal tract. While C-phenyl D-glucitol derivative SGL5213 has been reported to be a potent intestinal SGLT1 inhibitor for use in the treatmen

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c53e76b57ae8cefeb1cfd90272f7183b
https://pubmed.ncbi.nlm.nih.gov/32611999

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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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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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Contribution of testosterone to the clock system in rat prostate mesenchyme cells

Autor: Hirotaka Tasaki, Masa-aki Hattori, Guiyan Chu, Nobuhiko Yamauchi, Izumi Misawa, Madoka Kawamura

Publikováno v: Andrology. 2:225-233

Circadian rhythms are modulated in a variety of peripheral tissues including the prostate, in which the mesenchyme and epithelium cells are controlled under androgens. Here, we investigated the testosterone regulation of core clock genes such as Bmal

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::67fed3a87d1f01db7526ebdd3c052680
https://doi.org/10.1111/j.2047-2927.2013.00161.x

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Isoquinoline derivatives as potent CRTH2 antagonists: Design, synthesis and SAR

Autor: Shunichi Wakahara, Tetsuo Takayama, Kayo Kimura, Daisuke Wakasugi, Takeshi Koami, Susumu Yamanobe, Kazuhito Watanabe, Yoshinori Sekiguchi, Madoka Kawamura, Rie Nishikawa-Shimono

Publikováno v: Bioorganic & Medicinal Chemistry. 21:7674-7685

In this study, we describe the synthesis and structure-activity relationship (SAR) of a series of isoquinoline chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2) antagonists. TASP0376377 (15-20), one of the most potent compou

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e0e97f796082063093622d80a8cef5d
https://doi.org/10.1016/j.bmc.2013.10.025

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Alterations of Circadian Clockworks During Differentiation and Apoptosis of Rat Ovarian Cells

Autor: Seiichi Hashimoto, Sayoko Narahara, Yongmei Xi, Miho Uchikawa, Yasufumi Shigeyoshi, Madoka Kawamura, Guiyan Chu, Kaoru Yoshida, Nobuhiko Yamauchi, Masa-aki Hattori

Publikováno v: Chronobiology International. 28:477-487

Ovarian development is related to cell proliferation, differentiation, and apoptosis of granulosa cells and luteal cells under the control of various modulators, including follicle-stimulating hormone (FSH), luteinizing hormone (LH), and growth facto

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::35904907eeea7aecffb5d3fad019f577
https://doi.org/10.3109/07420528.2011.589933

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Down-Regulation of Circadian Clock GenePeriod 2in Uterine Endometrial Stromal Cells of Pregnant Rats During Decidualization

Autor: Nobuhiko Yamauchi, Miho Uchikawa, Madoka Kawamura, Masa-aki Hattori

Publikováno v: Chronobiology International. 28:1-9

Circadian rhythms are modulated in a variety of peripheral tissues, including in the uterus where endometrial stromal cells (UESCs) undergo proliferation and differentiation (decidualization) during gestation. Here the authors focused on circadian rh

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8732dbc848d546b6e1fad9019cf7fab9
https://doi.org/10.3109/07420528.2010.522289

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Isoquinoline derivatives as potent, selective, and orally active CRTH2 antagonists

Autor: Daisuke Wakasugi, Rie Nishikawa-Shimono, Kazuhito Watanabe, Yoshinori Sekiguchi, Madoka Kawamura, Masahumi Kawanishi, Yumiko Asakura, Tetsuo Takayama, Akiko Takaoka

Publikováno v: Chemicalpharmaceutical bulletin. 62(6)

Synthesis and structure-activity relationship of a novel series of isoquinoline CRTH2 antagonists bearing a methylene linker between the isoquinoline and benzamide moieties were described. Optimization focusing on the substituents of the benzamide po

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bb997ed88d7cbcfdd371e41398e71eac
https://pubmed.ncbi.nlm.nih.gov/24881658

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ChemInform Abstract: Isoquinoline Derivatives as Potent CRTH2 Receptor Antagonists: Synthesis and SAR

Autor: Kazuhito Watanabe, Daisuke Wakasugi, Kayo Matsumoto, Shunichi Wakahara, Tetsuo Takayama, Yoshinori Sekiguchi, Madoka Kawamura, Takeshi Koami, Rie Nishikawa-Shimono

Publikováno v: ChemInform. 43

The most potent compound, TASP0376377 (I) shows good CRTH2 antagonist potency, as well as sufficient selectivity for binding to CRTH2 over the DP1 prostanoid receptor and COX-1 and COX-2 enzymes.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8cb93fe26ec07de5685ab08f645f274e
https://doi.org/10.1002/chin.201238144

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