Search Results - "Kori, Masakuni"

A novel glycogen synthase kinase‐3 inhibitor 2‐methyl‐5‐(3‐{4‐[(S )‐methylsulfinyl]phenyl}‐1‐benzofuran‐5‐yl)‐1,3,4‐oxadiazole decreases tau phosphorylation and ameliorates cognitive deficits in a transgenic model of Alzheimer’s disease by Onishi, Tomohiro, Iwashita, Hiroki, Uno, Yumiko, Kunitomo, Jun, Saitoh, Morihisa, Kimura, Eiji, Fujita, Hisashi, Uchiyama, Noriko, Kori, Masakuni, Takizawa, Masayuki

“…J. Neurochem. (2011) 10.1111/j.1471‐4159.2011.07532.x Alzheimer’s disease (AD) is a neurodegenerative disorder leading to a progressive loss of cognitive…”
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Discovery of Novel, Highly Potent, and Selective Quinazoline-2-carboxamide-Based Matrix Metalloproteinase (MMP)-13 Inhibitors without a Zinc Binding Group Using a Structure-Based Design Approach by Nara, Hiroshi, Sato, Kenjiro, Naito, Takako, Mototani, Hideyuki, Oki, Hideyuki, Yamamoto, Yoshio, Kuno, Haruhiko, Santou, Takashi, Kanzaki, Naoyuki, Terauchi, Jun, Uchikawa, Osamu, Kori, Masakuni

“…Matrix metalloproteinase-13 (MMP-13) has been implicated to play a key role in the pathology of osteoarthritis. On the basis of X-ray crystallography, we…”
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Design and synthesis of 1-(1-benzothiophen-7-yl)-1H-pyrazole, a novel series of G protein-coupled receptor 52 (GPR52) agonists by Nakahata, Takashi, Tokumaru, Kazuyuki, Ito, Yoshiteru, Ishii, Naoki, Setoh, Masaki, Shimizu, Yuji, Harasawa, Toshiya, Aoyama, Kazunobu, Hamada, Teruki, Kori, Masakuni, Aso, Kazuyoshi

“…[Display omitted] G-protein-coupled receptor 52 (GPR52) is classified as an orphan Gs-coupled G-protein-coupled receptor. GPR52 cancels dopamine D2 receptor…”
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Discovery of the First Potent and Orally Available Agonist of the Orphan G‑Protein-Coupled Receptor 52 by Setoh, Masaki, Ishii, Naoki, Kono, Mitsunori, Miyanohana, Yuhei, Shiraishi, Eri, Harasawa, Toshiya, Ota, Hiroyuki, Odani, Tomoyuki, Kanzaki, Naoyuki, Aoyama, Kazunobu, Hamada, Teruki, Kori, Masakuni

“…G-protein-coupled receptor 52 (GPR52) is an orphan Gs-coupled G-protein-coupled receptor. GPR52 inhibits dopamine D2 receptor signaling and activates dopamine…”
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Enantioselective Synthesis of the Novel Chiral Sulfoxide Derivative as a Glycogen Synthase Kinase 3β Inhibitor by Saitoh, Morihisa, Kunitomo, Jun, Kimura, Eiji, Yamano, Toru, Itoh, Fumio, Kori, Masakuni

“…Glycogen synthase kinase 3β (GSK-3β) inhibitors are expected to be attractive therapeutic agents for the treatment of Alzheimer's disease (AD). Recently we…”
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Enantioselective synthesis of the novel chiral sulfoxide derivative as a glycogen synthase kinase 3beta inhibitor by Saitoh, Morihisa, Kunitomo, Jun, Kimura, Eiji, Yamano, Toru, Itoh, Fumio, Kori, Masakuni

“…Glycogen synthase kinase 3beta (GSK-3beta) inhibitors are expected to be attractive therapeutic agents for the treatment of Alzheimer's disease (AD). Recently…”
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Design, synthesis, and biological activity of novel, potent, and highly selective fused pyrimidine-2-carboxamide-4-one-based matrix metalloproteinase (MMP)-13 zinc-binding inhibitors by Nara, Hiroshi, Sato, Kenjiro, Kaieda, Akira, Oki, Hideyuki, Kuno, Haruhiko, Santou, Takashi, Kanzaki, Naoyuki, Terauchi, Jun, Uchikawa, Osamu, Kori, Masakuni

“…[Display omitted] Matrix metalloproteinase-13 (MMP-13), a member of the collagenase family of enzymes, has been implicated to play a key role in the pathology…”
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Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach by Nara, Hiroshi, Kaieda, Akira, Sato, Kenjiro, Naito, Takako, Mototani, Hideyuki, Oki, Hideyuki, Yamamoto, Yoshio, Kuno, Haruhiko, Santou, Takashi, Kanzaki, Naoyuki, Terauchi, Jun, Uchikawa, Osamu, Kori, Masakuni

“…On the basis of a superposition study of X-ray crystal structures of complexes of quinazoline derivative 1 and triazole derivative 2 with matrix…”
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Syntheses of (4,1-Benzoxazepine-3-ylidene)acetic Acid Derivatives and Their Inhibition of Squalene Synthase by Miki, Takashi, Kori, Masakuni, Tozawa, Ryu-ichi, Nakamura, Masahira, Sugiyama, Yasuo, Yukimasa, Hidefumi

“…The (3,5-trans)-7-chloro-5-(2-chlorophenyl)-2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepine-3-acetic acid derivatives 1 have been previously identified as potent…”
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Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: Highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site by Nara, Hiroshi, Sato, Kenjiro, Naito, Takako, Mototani, Hideyuki, Oki, Hideyuki, Yamamoto, Yoshio, Kuno, Haruhiko, Santou, Takashi, Kanzaki, Naoyuki, Terauchi, Jun, Uchikawa, Osamu, Kori, Masakuni

“…On the basis of X-ray co-crystal structures of matrix metalloproteinase-13 (MMP-13) in complex with its inhibitors, our structure-based drug design (SBDD)…”
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2-{3-[4-(Alkylsulfinyl)phenyl]-1-benzofuran-5-yl}-5-methyl-1,3,4-oxadiazole Derivatives as Novel Inhibitors of Glycogen Synthase Kinase-3β with Good Brain Permeability by Saitoh, Morihisa, Kunitomo, Jun, Kimura, Eiji, Iwashita, Hiroki, Uno, Yumiko, Onishi, Tomohiro, Uchiyama, Noriko, Kawamoto, Tomohiro, Tanaka, Toshimasa, Mol, Clifford D, Dougan, Douglas R, Textor, Garret P, Snell, Gyorgy P, Takizawa, Masayuki, Itoh, Fumio, Kori, Masakuni

“…Glycogen synthase kinase 3β (GSK-3β) inhibition is expected to be a promising therapeutic approach for treating Alzheimer’s disease. Previously we reported a…”
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Design and Synthesis of Benzimidazoles As Novel Corticotropin-Releasing Factor 1 Receptor Antagonists by Mochizuki, Michiyo, Kori, Masakuni, Kobayashi, Katsumi, Yano, Takahiko, Sako, Yuu, Tanaka, Maiko, Kanzaki, Naoyuki, Gyorkos, Albert C, Corrette, Christopher P, Cho, Suk Young, Pratt, Scott A, Aso, Kazuyoshi

“…Benzazole derivatives with a flexible aryl group bonded through a one-atom linker as a new scaffold for a corticotropin-releasing factor 1 (CRF1) receptor…”
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Microbial Enantioselective Ester Hydrolysis for the Preparation of Optically Active 4,1-Benzoxazepine-3-acetic Acid Derivatives as Squalene Synthase Inhibitors by Tarui, Naoki, Nakahama, Kazuo, Nagano, Yoichi, Izawa, Motowo, Matsumoto, Kiyoharu, Kori, Masakuni, Nagata, Toshiaki, Miki, Takashi, Yukimasa, Hidefumi

“…Microbial enantioselective ester hydrolysis for the preparation of optically active (3R, 5S)-(−)-5-phenyl-4,1-benzoxazepine-3-acetic acid derivatives as potent…”
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Synthesis, SAR study, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase (FAAH) inhibitors by Kono, Mitsunori, Matsumoto, Takahiro, Kawamura, Toru, Nishimura, Atsushi, Kiyota, Yoshihiro, Oki, Hideyuki, Miyazaki, Junichi, Igaki, Shigeru, Behnke, Craig A., Shimojo, Masato, Kori, Masakuni

“…A series of piperazine ureas was designed, synthesized, and evaluated for their potential as novel orally available fatty acid amide hydrolase (FAAH)…”
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Design, synthesis, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase inhibitors by Kono, Mitsunori, Matsumoto, Takahiro, Imaeda, Toshihiro, Kawamura, Toru, Fujimoto, Shinji, Kosugi, Yohei, Odani, Tomoyuki, Shimizu, Yuji, Matsui, Hideki, Shimojo, Masato, Kori, Masakuni

“…A series of piperazine ureas were designed, synthesized, and evaluated for their potential as novel orally efficacious fatty acid amide hydrolase (FAAH)…”
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Efficacy of a novel, orally active GSK-3 inhibitor 6-Methyl-N-[3-[[3-(1-methylethoxy)propyl]carbamoyl]-1H-pyrazol-4-yl]pyridine-3-carboxamide in tau transgenic mice by Uno, Yumiko, Iwashita, Hiroki, Tsukamoto, Tetsuya, Uchiyama, Noriko, Kawamoto, Tomohiro, Kori, Masakuni, Nakanishi, Atsushi

“…Abstract Neurofibrillary tangles (NFTs) composed of hyperphosphorylated and aggregated tau are common pathological characteristics in Alzheimer's disease (AD)…”
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Discovery of a 7-arylaminobenzimidazole series as novel CRF1 receptor antagonists by Mochizuki, Michiyo, Kori, Masakuni, Kono, Mitsunori, Yano, Takahiko, Sako, Yuu, Tanaka, Maiko, Kanzaki, Naoyuki, Gyorkos, Albert C., Corrette, Christopher P., Aso, Kazuyoshi

“…[Display omitted] A promising lead compound 1 of a benzimidazole series has been identified as a corticotropin-releasing factor 1 (CRF1) receptor antagonist…”
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A novel glycogen synthase kinase-3 inhibitor 2-methyl-5-(3-{4-[(S)-me thylsulfinyl]phenyl}-1-benzofuran-5-yl)-1,3,4-oxadiazole decreases tau phosphorylation and ameliorates cognitive deficits in a transgenic model of Alzheimer's disease by Onishi, Tomohiro, Iwashita, Hiroki, Uno, Yumiko, Kunitomo, Jun, Saitoh, Morihisa, Kimura, Eiji, Fujita, Hisashi, Uchiyama, Noriko, Kori, Masakuni, Takizawa, Masayuki

“…Alzheimer's disease (AD) is a neurodegenerative disorder leading to a progressive loss of cognitive function and is pathologically characterized by senile…”
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Total Synthesis of Rapamycin by Ley, Steven V., Tackett, Miles N., Maddess, Matthew L., Anderson, James C., Brennan, Paul E., Cappi, Michael W., Heer, Jag P., Helgen, Céline, Kori, Masakuni, Kouklovsky, Cyrille, Marsden, Stephen P., Norman, Joanne, Osborn, David P., Palomero, María Á., Pavey, John B. J., Pinel, Catherine, Robinson, Lesley A., Schnaubelt, Jürgen, Scott, James S., Spilling, Christopher D., Watanabe, Hidenori, Wesson, Kieron E., Willis, Michael C.

“…Rapamycin (1) is a macrocyclic natural product, established as a potent immunosuppressant and currently of interest to the scientific community as the…”
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P2‐534: Efficacy of a novel, orally active GSK‐3 Inhibitor 6‐Methyl‐N‐[3‐[[3‐(1‐methylethoxy)propyl]carbamoyl]‐1H‐pyrazol‐4‐yl]pyridine‐3‐carboxamide in tau transgenic mice by Uno, Yumiko, Iwashita, Hiroki, Tsukamoto, Tetsuya, Uchiyama, Noriko, Kawamoto, Tomohiro, Kori, Masakuni, Nakanishi, Atsushi

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