Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Akito, Kakuuchi"'
Autor:
Yoshiyuki Aratani, Hidekazu Matsuya, Koji Yoshida, Masato Higashino, Atsushi Naganawa, Hiroyuki Takeda, Akihiro Kinoshita, Keisuke Hanada, Kazuyuki Ohmoto, Akito Kakuuchi
Publikováno v:
Bioorganic & Medicinal Chemistry. 26:200-214
A highly potent and well-balanced dual agonist for the EP2 and EP3 receptors is described. Optimization of the lead compound was accomplished in consideration of the relative agonist activity against each EP subtype receptor and the pharmacokinetic p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::56e5a038bf3b1ac9687e5fd070824092
https://doi.org/10.1016/j.bmc.2017.11.035
https://doi.org/10.1016/j.bmc.2017.11.035
Autor:
Hidekazu Matsuya, Yoshiyuki Aratani, Masato Higashino, Akihiro Kinoshita, Kazuyuki Ohmoto, Akito Kakuuchi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:1016-1019
The cyclic carbamate derivatives, 2-{[2-((4S)-4-{(1E,3R)-8-fluoro-3-hydroxy-4,4-dimethyl-1-octenyl}-2-oxo-1,3-oxazolidin-3-yl)ethyl]sulfanyl}-1,3-thiazole-4-carboxylic acid (5) and 2-{[2-((4S)-4-{(1E,3R)-3-[1-(4-fluorobutyl)cyclobutyl]-3-hydroxy-1-pr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1a560699e3534685aede696fd825be5c
https://doi.org/10.1016/j.bmcl.2015.12.039
https://doi.org/10.1016/j.bmcl.2015.12.039
Autor:
Kazuhiro Otsuki, Hiroshi Yamamoto, Haruto Kurata, Ai Hashimoto, Koji Shinozaki, Takeshi Matsushita, Takuya Seko, Yoshiyuki Yamaura, Tetsuya Sekiguchi, Kensuke Kusumi, Akito Kakuuchi, Atsushi Naganawa
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:1209-1213
The structure of the S1P2 antagonist 1 has been modified with the aim of improving its oral bioavailability. The chemical modification of the alkyl chain and carboxylic acid moieties of 1 led to significant improvements in the oral exposure of compou
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d25a2df178b653cedb5d031676d280d5
https://doi.org/10.1016/j.bmcl.2016.01.031
https://doi.org/10.1016/j.bmcl.2016.01.031
Autor:
Hideyuki Ueda, Ai Hashimoto, Tetsuya Sekiguchi, Kazuhiro Otsuki, Takuya Seko, Kensuke Kusumi, Haruto Kurata, Akito Kakuuchi, Yoshiyuki Yamaura, Atsushi Naganawa, Koji Shinozaki, Takeshi Matsushita
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:4387-4392
Our initial lead compound 2 was modified to improve its metabolic stability. The resulting compound 5 showed excellent metabolic stability in rat and human liver microsomes. We subsequently designed and synthesized a hybrid compound of 5 and the 1,3-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fee7eda0e3ed88ff58ed6cf0b673fbb6
https://doi.org/10.1016/j.bmcl.2015.09.022
https://doi.org/10.1016/j.bmcl.2015.09.022
Autor:
Akito Kakuuchi, Haruto Kurata, Kazuhiro Otsuki, Tetsuya Sekiguchi, Atsushi Naganawa, Koji Shinozaki, Takeshi Matsushita, Kensuke Kusumi, Takuya Seko, Kanaji Toshiya
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:1479-1482
The structure–activity relationships of a novel series of sphingosine-1-phosphate receptor antagonists have been examined in detail. The initial hit compound 1 was modified through synthesis to improve its S1P2 activity. The synthesis of a series o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe897b0e5487ff42688c85ffea02bdb8
https://doi.org/10.1016/j.bmcl.2015.02.029
https://doi.org/10.1016/j.bmcl.2015.02.029
Autor:
Akihiro, Kinoshita, Masato, Higashino, Koji, Yoshida, Yoshiyuki, Aratani, Akito, Kakuuchi, Keisuke, Hanada, Hiroyuki, Takeda, Atsushi, Naganawa, Hidekazu, Matsuya, Kazuyuki, Ohmoto
Publikováno v:
Bioorganicmedicinal chemistry. 26(1)
A highly potent and well-balanced dual agonist for the EP
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::cecf82fc6035858f7d7798ca4b5c57c2
https://pubmed.ncbi.nlm.nih.gov/29203142
https://pubmed.ncbi.nlm.nih.gov/29203142
Publikováno v:
Tetrahedron. 60:1293-1299
The 1,4-conjugated addition of alkenylzirconocene chloride complexes to α,β-enones, α,β-enoic acid esters, and α,β-enoic acid amides can be efficiently achieved by the use of [RhCl(cod)] 2 catalyst. A high diastereoselectivity (95% yield, 90% d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7683b9df7d1d8fe355e1fdd829d23c06
https://doi.org/10.1016/j.tet.2003.08.073
https://doi.org/10.1016/j.tet.2003.08.073
Publikováno v:
Tetrahedron Letters. 44:923-926
[RhCl(COD)] 2 (2 mol%) catalyzed reactions of alkenylzirconocene chloride complexes to N -Ts, -PO(OEt) 2 and COOR aldimine derivatives were efficiently carried out in dioxane at room temperature to give allylic amine derivatives in excellent yields.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d50e5f181c102d45b02b1e242bd243a3
https://doi.org/10.1016/s0040-4039(02)02767-3
https://doi.org/10.1016/s0040-4039(02)02767-3
Publikováno v:
Tetrahedron. 58:7559-7571
Acylzirconocene chlorides reacted with α,β-unsaturated ketones (α,β-enone or -ynone) to give regioselectively 1,2- or 1,4-products under Pd-catalyzed conditions. In the reactions of α,β-enones, excellent regioselectivity was attained by the cho
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff21725c04b53d717fb62378c143fec0
https://doi.org/10.1016/s0040-4020(02)00857-8
https://doi.org/10.1016/s0040-4020(02)00857-8
Publikováno v:
Tetrahedron Letters. 41:7525-7528
Reactions of α,β-unsaturated acylzirconocene chloride with nucleophiles showed novel bimodal reactivity at the β- and acyl carbons depending upon the nucleophile employed, and the formation of ketone α,β-dianionic species was also observed.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d8d2cd180ecf5138d84c30ebb069aafc
https://doi.org/10.1016/s0040-4039(00)01291-0
https://doi.org/10.1016/s0040-4039(00)01291-0