Výsledky vyhledávání - "Tomoya Kotake"

Lead Optimization and Avoidance of Reactive Metabolite Leading to PCO371, a Potent, Selective, and Orally Available Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist

Autor: Yoshiaki Watanabe, Haruhiko Sato, Hidetomo Kitamura, Tomoya Kotake, Yoshikazu Nishimura, Masaru Shimizu, Takashi Emura, Kotaro Ogawa, Toru Esaki, Toshito Nakagawa, Akemi Mizutani, Yoshiyuki Furuta, Shinichi Arai, Hiroshi Noda, Masateru Ohta, Tatsuya Tamura, Yoshiaki Isshiki

Publikováno v: Journal of Medicinal Chemistry. 63:5089-5099

We have previously shown that the oral administration of the small molecule hPTHR1 agonist PCO371 and its lead compound, 1 (CH5447240) results in PTH-like calcemic and hypophostemic activity in thyroparathyroidectomized rats. However, 1 was converted

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e990e3b015767e8e07afcf1625e08030
https://doi.org/10.1021/acs.jmedchem.9b01743

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Development of a Novel Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist (CH5447240), a Potent and Orally Available Small Molecule for Treatment of Hypoparathyroidism

Autor: Masaru Shimizu, Yoshikazu Nishimura, Masateru Ohta, Toshito Nakagawa, Yoshiyuki Furuta, Naoki Okamoto, Yoshiaki Isshiki, Haruhiko Sato, Yoshiaki Watanabe, Hitoshi Saito, Hiroshi Noda, Tatsuya Tamura, Tomoya Kotake, Toru Esaki

Publikováno v: Journal of Medicinal Chemistry. 61:5949-5962

During the course of derivatization of HTS hit 4a, we have identified a novel small-molecule hPTHR1 agonist, 1-(3,5-dimethyl-4-(2-((2-((1R,4R)-4-methylcyclohexyl)-4-oxo-1,3,8-triazaspiro[4.5]dec-1-en-8-yl)sulfonyl)ethyl)phenyl)-1-methylurea (CH544724

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5ee5e48d9dacf5c4280be8d1ffd84fb9
https://doi.org/10.1021/acs.jmedchem.8b00182

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Design and synthesis of a new polymer-supported Evans-type oxazolidinone: an efficient chiral auxiliary in the solid-phase asymmetric alkylation reactions

Autor: Tooru Kimura, Tomoya Kotake, S. Rajesh, Yoshie Mukai, Yoshiaki Kiso, Yuka Takiguchi, Yoshio Hayashi

Publikováno v: Tetrahedron. 61:3819-3833

Wang resin-supported Evans' chiral auxiliary (23) was designed based on a novel polymer-anchoring strategy, which utilizes the 5-position of the oxazolidinone ring, and its new synthetic route applicable to multi-gram preparation in just a day was de

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d6deff5c527cfb77ec2ac27e516f8e93
https://doi.org/10.1016/j.tet.2005.01.135

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A new polymer-supported Evans-type chiral auxiliary derived from α-hydroxy-β-amino acid, phenylnorstatine: synthesis and application in solid-phase asymmetric alkylation reactions

Autor: Yoshiaki Kiso, Tooru Kimura, Yoshio Hayashi, S. Rajesh, Mitsuhiro Ueda, Yoshie Mukai, Tomoya Kotake

Publikováno v: Tetrahedron Letters. 45:3651-3654

Based on a new anchoring strategy, a polymer-supported chiral oxazolidinone was prepared starting from (2R,3S)-3-amino-2-hydroxy-4-phenylbutanoic acid (phenylnorstatine, Pns) and Wang resin. Solid-phase asymmetric alkylation on this resin proceeded i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::70aa6068f324d9fe7728267f67cc6504
https://doi.org/10.1016/j.tetlet.2004.03.043

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Asymmetric total synthesis of 9-methoxystrobilurin K

Autor: Daiju Hasegawa, Tomoya Kotake, Yasuyuki Aiba, Koh Nagasawa, Hiromi Uchiro, Susumu Kobayashi

Publikováno v: Tetrahedron Letters. 42:4531-4534

Asymmetric total synthesis of a potent antifungal and cytostatic 9-methoxystrobilurin K was achieved by developing a convergent and versatile synthetic route.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d17c544856499c5d2ee2f49e7dee2122
https://doi.org/10.1016/s0040-4039(01)00812-7

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An expedient synthesis of Nα-protected-l-tetrahydrofuranylglycine and its application in the synthesis of novel substrate based inhibitors of HIV-1 protease

Autor: Yoshio Hayashi, S. Rajesh, Tooru Kimura, Yoshiaki Kiso, Tomoya Kotake, Ei'ichi Ami

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 12:3615-3617

Z- and Fmoc- l -tetrahydrofuranylglycines have been obtained from l -vinylglycine through dipolar cycloaddition reaction, and its Fmoc derivative has been applied in the synthesis of modified S9 and S10 substrates of HIV-1 protease. These compounds m

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2d65c81e75dfd0c67d9fdd54d292861e
https://doi.org/10.1016/s0960-894x(02)00781-3

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Development of Wang Resin Supported Evans-type Oxazolidinone for Asymmetric Reaction

Autor: S. Rajesh, Tooru Kimura, Yoshiaki Kiso, Tomoya Kotake, Yoshio Hayashi

Publikováno v: Understanding Biology Using Peptides ISBN: 9780387265698

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::33ada2722590972a2ec89a7f035e3536
https://doi.org/10.1007/978-0-387-26575-9_32

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ChemInform Abstract: Asymmetric Total Synthesis of 9-Methoxystrobilurin K

Autor: Koh Nagasawa, Hiromi Uchiro, Susumu Kobayashi, Yasuyuki Aiba, Tomoya Kotake, Daiju Hasegawa

Publikováno v: ChemInform. 32

Asymmetric total synthesis of a potent antifungal and cytostatic 9-methoxystrobilurin K was achieved by developing a convergent and versatile synthetic route.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::2b0ef78b99e1470b0dc02f9c65579087
https://doi.org/10.1002/chin.200139241

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Remarkable influence of the aromatic substructure in 9-methoxystrobilurin derivatives on their antifungal activity

Autor: Koh Nagasawa, Hiromi Uchiro, Satoshi Ōmura, Tomoya Kotake, Daiju Hasegawa, Kazuhiko Otoguro, Tomohiro Sawa, Susumu Kobayashi, Yoshitsugu Sugiura

Publikováno v: Bioorganicmedicinal chemistry letters. 12(19)

9-Methoxystrobilurin-type beta-methoxyacrylate antibiotics (MOSBs) having various aromatic substructures were synthesized. The antifungal activity of the synthesized MOSBs against pathogenic and non-pathogenic fungi was examined, and the obtained res

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::de9386897bb2ebc555d595ac2acee504
https://pubmed.ncbi.nlm.nih.gov/12217357

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