Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Hidekazu Tokuhara"'
Autor:
Shuhei Ikeda, Hideyuki Sugiyama, Hidekazu Tokuhara, Masataka Murakami, Minoru Nakamura, Yuya Oguro, Jumpei Aida, Nao Morishita, Satoshi Sogabe, Douglas R. Dougan, Sean C. Gay, Ling Qin, Naoto Arimura, Yasuko Takahashi, Masako Sasaki, Yusuke Kamada, Kazunobu Aoyama, Kouya Kimoto, Makoto Kamata
Publikováno v:
Journal of Medicinal Chemistry. 64:11014-11044
The therapeutic potential of monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases has attracted attention worldwide. However, the availability of reversible-type inhibitor is still limited to clarify the pharmacologica
Autor:
Craig A. Behnke, Ray Kanagawa, Koji Watanabe, Keisuke Matsuda, Yumiko Kajimoto, Yasuhiro Imaeda, Koichi Iwanaga, Naohiro Taya, Keiji Kusumoto, Takanobu Kuroita, Hidekazu Tokuhara, Mitsuyo Kondo, Gyorgy Snell, Yoshiyuki Fukase
Publikováno v:
Bioorganic & Medicinal Chemistry. 26:3261-3286
We previously identified 2-tert-butyl-4-[(3-methoxypropyl)amino]-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]pyrimidine-5-carboxamide 3 as a potent renin inhibitor. Since 3 showed unacceptably low bioavailability (BA) in ra
Autor:
Isaac Hoffman, Masaharu Nakayama, Masato Yoshida, Yusuke Sasaki, Hua Zou, Hideyuki Nakagawa, Atsutoshi Okabe, Yusuke Ohba, Robert J. Skene, Hidekazu Tokuhara
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(5)
Herein we report an efficient method for the synthesis of a highly functionalized 2-pyrrolidinone, tert-butyl 3-cyano-3-cyclopropyl-2-oxopyrrolidine-4-carboxylate, from readily available starting materials. Utility of this compound was demonstrated i
Autor:
Junya Shirai, Yoshiyuki Fukase, Tetsuji Kawamoto, Mitsunori Kono, Tsuneo Oda, Mikio Shirasaki, Yasushi Fujitani, Hiroyuki Watanabe, Hideyuki Nakagawa, Keiko Uga, Michiko Tawada, Naohiro Taya, Akira Shibata, Takashi Imada, Yoshihide Tomata, Masashi Yamasaki, Tomoya Yukawa, Shoji Fukumoto, Hidekazu Tokuhara, Satoshi Yamamoto, Naoki Ishii, Atsuko Ochida, Yoshihiro Banno
Publikováno v:
Bioorganic & Medicinal Chemistry. 26:470-482
A series of tetrahydroisoquinoline derivatives were designed, synthesized, and evaluated for their potential as novel orally efficacious retinoic acid receptor-related orphan receptor-gamma t (RORγt) inverse agonists for the treatment of Th17-driven
Autor:
Hidekazu Tokuhara, Gyorgy Snell, Keiji Kusumoto, Craig A. Behnke, Mitsuyo Kondo, Yasuhiro Imaeda, Yumiko Kajimoto, Yoshiyuki Fukase, Takanobu Kuroita, Ray Kanagawa
Publikováno v:
ACS Medicinal Chemistry Letters
The aspartic proteinase renin is an attractive target for the treatment of hypertension and cardiovascular/renal disease such as chronic kidney disease and heart failure. We introduced an S1′ site binder into the lead compound 1 guided by structure
Autor:
Keiko Igaki, Yoshihiro Banno, Tsuneo Oda, Akira Shibata, Bi-Ching Sang, Masashi Yamasaki, Hideyuki Nakagawa, Atsuko Ochida, Hidekazu Tokuhara, Kazuko Yonemori, Junya Shirai, Satoshi Yamamoto, Yoshiyuki Fukase, Gyorgy Snell, Shinichi Masada, Tomoya Yukawa, Yoshi Nara, Isaac Hoffman, Tetsuji Kawamoto, Mitsunori Kono, Noboru Tsuchimori, Yoshiki Nakamura, Keiko Uga, Takashi Imada, Naohiro Taya, Robert J. Skene
Publikováno v:
Journal of medicinal chemistry. 61(7)
A series of tetrahydronaphthyridine derivatives as novel RORγt inverse agonists were designed and synthesized. We reduced the lipophilicity of tetrahydroisoquinoline compound 1 by replacement of the trimethylsilyl group and SBDD-guided scaffold exch
Autor:
Hidekazu Tokuhara, Naoki Ogura, Araki Masuyama, Kanako Ono, Hye‐Sook Kim, Masatomo Nojima, Y. Hamada, Yusuke Wataya
Publikováno v:
Journal of Medicinal Chemistry. 45:1374-1378
Of several bis(alkyldioxy)alkanes and the related acyclic peroxides prepared in this study, 1,1-bis(methyldioxy)cyclododecane showed the most notable antimalarial activity particularly in vivo (almost a half of that of artemisinin).
Autor:
Mitsunori Kono, Atsuko Ochida, Tsuneo Oda, Takashi Imada, Yoshihiro Banno, Naohiro Taya, Shinichi Masada, Tetsuji Kawamoto, Kazuko Yonemori, Yoshi Nara, Yoshiyuki Fukase, Tomoya Yukawa, Hidekazu Tokuhara, Skene, Robert, Bi-Ching Sang, Hoffman, Isaac D., Snell, Gyorgy P., Keiko Uga, Akira Shibata, Keiko Igaki
Publikováno v:
Journal of Medicinal Chemistry; 4/12/2018, Vol. 61 Issue 7, p2973-2988, 16p
Autor:
Natsuki Tanigawa, Masatomo Nojima, Hikoya Hayatsu, Masayuki Morita, Yukari Nakase, Akiko Hiramoto, Yusuke Wataya, Kazutaka Higaki, Osamu Hiraoka, Masahiro Matsumoto, Hidekazu Tokuhara, Araki Masuyama, Yuka Komichi, Satoru Kawai, Akira Sato, Hye Sook Kim, Kazuyuki Hiramoto
Publikováno v:
Parasitology international. 60(4)
Malaria is one of the world's deadliest diseases and is becoming an increasingly serious problem as malaria parasites develop resistance to most of the antimalarial drugs used today. We previously reported the in vitro and in vivo antimalarial potenc
Publikováno v:
ChemInform. 34
Ozonolysis of (alkenyldioxy)cyclododecyl hydroperoxides in trifluoroethanol gave a separable mixture of the corresponding alpha-hydroperoxy- and alpha-hydroxy-substituted spiro-tetraoxacycloalkanes with ring sizes in the range 7-12. Dehydration of th