Zobrazeno 1 - 10
of 28
pro vyhledávání: '"Hiroshi Miyazoe"'
Autor:
Akane Ishihara, Shigeru Tokita, Satoru Ito, Hiroshi Miyazoe, Masahiko Ito, Minoru Moriya, Kazuho Nakase, Kaori Kamijo, Hiroko Matsushita, Minoru Kameda, Kouta Masutani, Etsuko Sekino, Akihiro Takezawa, Norihiro Takenaga, Takehiro Fukami, Akio Kanatani, Nagaaki Sato, Makoto Ando, Junko Ito, Takao Suzuki
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5339-5345
Optimization of the lead 2a led to the identification of a novel diarylketoxime class of melanin-concentrating hormone 1 receptor (MCH-1R) antagonists. Our focus was directed toward improvement of hERG activity and metabolic stability. The representa
Autor:
Takashi Yoshizumi, Hisashi Ohta, Hiroshi Miyazoe, Kensuke Kobayashi, Masanori Asai, Satoshi Ozaki, Yasuyuki Ishii, Osamu Okamoto, Hiroki Sakoh, Takeshi Tani, Mioko Hirayama, Tomohiro Tsujita, Minaho Uchiyama, Hirokatsu Ito, Hirobumi Takahashi, Yasushi Nagatomi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:3627-3631
The synthesis and biological evaluation of new potent opioid receptor-like 1 antagonists are presented. A structure-activity relationship (SAR) study of arylpyrazole lead compound 1 obtained from library screening identified compound 31, (1S,3R)-N-{[
Autor:
Yasuyuki Ishii, Hiroshi Miyazoe, Akio Ohno, Takeshi Tanaka, Takanobu Mochidome, Hirobumi Takahashi, Mioko Hirayama, Hiroshi Kawamoto, Kiyoshi Tadano, Masanori Asai, Izumi Yamamoto, Takashi Yoshizumi, Tetsuya Kato, Kensuke Kobayashi, Takahiro Fukuroda, Takeshi Tani, Osamu Okamoto, Minaho Uchiyama, Hiroshi Nakashima, Satoshi Ozaki, Satoru Ito, Hisashi Ohta, Atsushi Shimizu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:3096-3099
The synthesis and biological evaluation of new potent opioid receptor-like 1 (ORL1) antagonists are presented. Conversion of the thioether linkage of the prototype [It is reported prior to this communication as a consecutive series.: Kobayashi, K.; K
Autor:
Satoshi Ozaki, Hiroshi Miyazoe, Hisashi Ohta, Masanori Asai, Hirobumi Takahashi, Osamu Okamoto, Hirokatsu Ito, Takashi Yoshizumi, Tomohiro Tsujita
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3778-3782
Based on reported structures, a focused library of biarylmethyl bound to the nitrogen atom of spiropiperidine was designed. Systematic modifications allowed the discovery of a synthetically feasible and highly potent ORL1 antagonist 37, 1'-{[1-(3-chl
Autor:
Takeshi Tani, Hisashi Ohta, Tetsuya Kato, Tomohiro Tsujita, Hirobumi Takahashi, Hirokatsu Ito, Mioko Hirayama, Kiyoshi Tadano, Tomoko Azuma-Kanoh, Hiroshi Kawamoto, Masato Chiba, Daisuke Ichikawa, Osamu Okamoto, Yuichi Sugimoto, Takahiro Fukuroda, Yoshihiro Shibata, Satoshi Ozaki, Takashi Yoshizumi, Shoki Okuda, Hiroshi Miyazoe, Yasuyuki Ishii
Publikováno v:
Journal of Medicinal Chemistry. 51:4021-4029
A series of compounds based on 7-{[4-(2-methylphenyl)piperidin-1-yl]methyl}-6,7,8,9-tetrahydro-5 H-cyclohepta[ b]pyridine-9-ol ( (-)-8b), a potent and selective opioid receptor-like 1 (ORL1) antagonist, was prepared and evaluated using structure-acti
Publikováno v:
Synthesis. :1593-1600
Development of a convenient and efficient synthetic route for functionalized tetrahydrocycloheptapyridines was accomplished by stepwise iodomethylation and subsequent radical ring expansion using a Bu 3 SnH/AIBN reaction system. Thus, 8- or 5-oxotetr
Publikováno v:
Tetrahedron Letters. 41:7517-7520
Acyl radicals generated from either acyl tellurides or alkyl tellurides and carbon monoxide react with isonitriles to give α-acyl-substituted imidoyl tellurides in good to excellent yield. Hydrolysis of the product under oxidative conditions provide
Publikováno v:
Tetrahedron Letters. 40:2343-2346
Glycosyl radicals generated from telluroglycosides react with a variety of alkynes to give the corresponding vinylic C -glycosides in good to excellent yields. The reaction takes place in an atom transfer manner to form vinyl telluride, and the resul
Publikováno v:
Tetrahedron Letters. 40:2339-2342
1-β-Telluroglycosides isomerize to α-isomers upon photolysis and thermolysis. The isomerization follows first-order reaction kinetics and proceeds through a glycosyl radical intermediate by homolytic CTe bond cleavage. The radicals so generated
Publikováno v:
Tetrahedron Letters. 40:2347-2350
Telluroglycosides react with isonitriles under photo-thermal conditions to give 1-telluroimidoylglycosides. The reaction proceeds by atom transfer radical reaction to form an imidic CTe bond, which can be substituted to a CC bond and CO bond