Výsledky vyhledávání - "Tetsuo Asaki"

Discovery of a novel class of 1,3-dioxane-2-carboxylic acid derivatives as subtype-selective peroxisome proliferator-activated receptor α (PPARα) agonists

Autor: Makoto Todo, Tomiyoshi Aoki, Tetsuo Asaki, Shinji Ohmachi, Kenji Kuwabara, Kohji Murakami, Yukiteru Sugiyama, Taisuke Hamamoto

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 18:2128-2132

A new series of 1,3-dioxane-2-carboxylic acid derivatives was synthesized and evaluated for agonist activity at human peroxisome proliferator-activated receptor (PPAR) subtypes. Structure-activity relationship studies led to the identification of 2-m

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5fa343fd698e8684a49e6f0eb0a4688c
https://doi.org/10.1016/j.bmcl.2008.01.086

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Structure–activity relationship study on the 6-membered heteroaromatic ring system of diphenylpyrazine-type prostacyclin receptor agonists

Autor: Yukiteru Sugiyama, Taisuke Hamamoto, Keiichi Kuwano, Tetsuo Asaki, Kenji Kuwabara, Tomoko Niwa

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 17:6588-6592

A series of prostacyclin receptor agonists was prepared by modifying the central heteroaromatic ring of lead compound 2 , and a docking study was performed to investigate their structure–activity relationships by using a homology-modeled structure

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::837597060713905d323bf359bd6dbdcc
https://doi.org/10.1016/j.bmcl.2007.09.066

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2-{4-[(5,6-Diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide (NS-304), an Orally Available and Long-Acting Prostacyclin Receptor Agonist Prodrug

Autor: Tetsuo Asaki, Kenji Kuwabara, Taisuke Hamamoto, Kaori Okubo, Tetsuhiro Yamada, Asami Hashino, Keiichi Kuwano

Publikováno v: Journal of Pharmacology and Experimental Therapeutics. 322:1181-1188

Prostacyclin (PGI(2)) and its analogs are useful for the treatment of various vascular disorders, but their half-lives are too short for widespread clinical application. To overcome this drawback, we have synthesized a novel diphenylpyrazine derivati

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::80a9f71c0f437a504068ecec82f3f97d
https://doi.org/10.1124/jpet.107.124248

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Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives

Autor: Hiroki Hayase, Shinsaku Itou, Tatsuya Horio, Tomohiro Hamasaki, Toshihiko Inoue, Tomoko Niwa, Tetsuo Asaki, Haruna Naito, Tatsushi Wakayama

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 17:2712-2717

To investigate why 3-substituted benzamide derivatives show dual inhibition of Abl and Lyn protein tyrosine kinases, we determined their inhibitory activities against Abl and Lyn, carried out molecular modeling, and conducted a structure-activity rel

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c8f869f000a245e129f7d5f0cea388e
https://doi.org/10.1016/j.bmcl.2007.03.002

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Design and synthesis of 3-substituted benzamide derivatives as Bcr-Abl kinase inhibitors

Autor: Masato Umehara, Tomoko Niwa, Masaya Higashioka, Yukiteru Sugiyama, Tetsuo Asaki, Taisuke Hamamoto, Haruna Naito

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 16:1421-1425

A series of 3-substituted benzamide derivatives structurally related to STI-571 (imatinib mesylate), a Bcr-Abl tyrosine kinase inhibitor used to treat chronic myeloid leukemia (CML), was prepared and evaluated for antiproliferative activity against t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3dafdf9265ba05f803620604a12708a6
https://doi.org/10.1016/j.bmcl.2005.11.042

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NS-187, a potent and selective dual Bcr-Abl/Lyn tyrosine kinase inhibitor, is a novel agent for imatinib-resistant leukemia

Autor: Takeshi Yuasa, Junya Kuroda, Yuri Kamitsuji, Eri Kawata, Kiyoshi Sato, Tomoko Niwa, Shinya Kimura, Asumi Yokota, Hidekazu Segawa, Tetsuo Asaki, Kazuko Hirabayashi, Taira Maekawa, Haruna Naruoka, Yohei Nakaya, Eishi Ashihara, Haruna Naito, Tatsushi Wakayama, Kimio Nasu

Publikováno v: Blood. 106:3948-3954

Although the Abelson (Abl) tyrosine kinase inhibitor imatinib mesylate has improved the treatment of breakpoint cluster region–Abl (Bcr-Abl)–positive leukemia, resistance is often reported in patients with advanced-stage disease. Although several

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e65e481dcc9d49213c195ecff04fc754
https://doi.org/10.1182/blood-2005-06-2209

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NS-187 (INNO-406), a Bcr-Abl/Lyn dual tyrosine kinase inhibitor

Autor: Tomoko Niwa, Tetsuo Asaki, Shinya Kimura

Publikováno v: Analytical Chemistry Insights
Analytical Chemistry Insights, Vol 2, Pp 93-106 (2007)

Protein kinases catalyze the transfer of the γ-phosphoryl group of adenosine triphosphate (ATP) to the hydroxyl groups of protein side chains, and they play critical roles in regulating cellular signal transduction and other biochemical processes. T

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6b8e4ec7ea03fedad2de7d3610c1be03
https://pubmed.ncbi.nlm.nih.gov/19662183

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Structure-activity studies on 1,3-dioxane-2-carboxylic acid derivatives, a novel class of subtype-selective peroxisome proliferator-activated receptor alpha (PPARalpha) agonists

Autor: Makoto Todo, Yukiteru Sugiyama, Tomiyoshi Aoki, Shinji Ohmachi, Kohji Murakami, Tetsuo Asaki, Kenji Kuwabara, Taisuke Hamamoto

Publikováno v: Bioorganicmedicinal chemistry. 16(2)

A series of 1,3-dioxane carboxylic acid derivatives was synthesized and evaluated for human PPAR transactivation activity. Structure-activity relationships on the phenyloxazole moiety of the lead compound 3 revealed that the introduction of small hyd

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f2866d3073594659655aca56a8f2dccf
https://pubmed.ncbi.nlm.nih.gov/17964792

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Synthesis and evaluation of N-acylsulfonamide and N-acylsulfonylurea prodrugs of a prostacyclin receptor agonist

Autor: Akio Nakamura, Tetsuhiro Yamada, Tetsuo Asaki

Publikováno v: Bioorganicmedicinal chemistry. 15(24)

N-Acylsulfonamide and N-acylsulfonylurea derivatives of the carboxylic acid prostacyclin receptor agonist 1 were synthesized and their potential as prodrug forms of the carboxylic acid was evaluated in vitro and in vivo. These compounds were converte

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0e5b517dee8969e9d28af029846e1057
https://pubmed.ncbi.nlm.nih.gov/17881233

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A novel selective peroxisome proliferator-activated receptor alpha agonist, 2-methyl-c-5-[4-[5-methyl-2-(4-methylphenyl)-4-oxazolyl]butyl]-1,3-dioxane-r-2-carboxylic acid (NS-220), potently decreases plasma triglyceride and glucose levels and modifies lipoprotein profiles in KK-Ay mice

Autor: Tomiyoshi Aoki, Junichi Yano, Makoto Todo, Kohji Murakami, Masatoshi Murai, Tetsuo Asaki, Kenji Kuwabara

Publikováno v: The Journal of pharmacology and experimental therapeutics. 309(3)

2-Methyl-c-5-[4-[5-methyl-2-(4-methylphenyl)-4-oxazolyl]butyl]-1,3-dioxane-r-2-carboxylic acid (NS-220) was newly synthesized and demonstrated to be a novel potent peroxisome proliferator-activated receptor alpha (PPARalpha) agonist with high subtype

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8c8fbae9d9e1dfb59c5c55ef4f138885
https://pubmed.ncbi.nlm.nih.gov/14982965

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