Search Results - "Kume, Masaharu"

Discovery of naldemedine: A potent and orally available opioid receptor antagonist for treatment of opioid-induced adverse effects by Inagaki, Masanao, Kume, Masaharu, Tamura, Yoshinori, Hara, Shinichiro, Goto, Yoshihisa, Haga, Nobuhiro, Hasegawa, Tsuyoshi, Nakamura, Takashi, Koike, Katsumi, Oonishi, Shuuichi, Kanemasa, Toshiyuki, Kai, Hiroyuki

“…[Display omitted] •We discovered a new chemotype, 7-carboxamide morphinan derivatives as opioid antagonist.•This chemotype is suitable for acting on…”
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Total Synthesis and Comparative Evaluation of Luzopeptin A−C and Quinoxapeptin A−C by Boger, Dale L, Ledeboer, Mark W, Kume, Masaharu, Searcey, Mark, Jin, Qing

“…Full details of the total syntheses of luzopeptin A−C and quinoxapeptin A−C, C 2-symmetric cyclic depsidecapeptides bearing two pendant heterocyclic…”
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Total Synthesis of Quinoxapeptin A-C: Establishment of Absolute Stereochemistry by Boger, Dale L., Ledeboer, Mark W., Kume, Masaharu, Jin, Qing

“…The relative and absolute stereochemistry of the naturally occurring potent HIV reverse transcriptase (RT) inhibitors 1 and 2, quinoxapeptin A and B, were…”
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Pyrrolinone derivatives as a new class of P2X3 receptor antagonists. Part 1: Initial structure-activity relationship studies of a hit from a high throughput screening by Tobinaga, Hiroyuki, Kameyama, Takayuki, Oohara, Miho, Kobayashi, Naotake, Ohdan, Masahide, Ishizuka, Natsuki, Kume, Masaharu, Tomari, Maki, Tanaka, Yoshikazu, Takahashi, Fumiyo, Kinoshita, Haruki, Shimada, Shinji, Shinohara, Shunji, Kai, Hiroyuki

“…[Display omitted] The P2X3 receptor is primarily expressed in the peripheral sensory nerves, and therefore, antagonists of this receptor may be useful for the…”
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Discovery of NR2B-selective antagonists via scaffold hopping and pharmacokinetic profile optimization by Anan, Kosuke, Masui, Moriyasu, Tazawa, Aya, Tomida, Minoru, Haga, Yoshihiro, Kume, Masaharu, Yamamoto, Shoichi, Shinohara, Shunji, Tsuji, Hiroki, Shimada, Shinji, Yagi, Shigenori, Hasebe, Nobuyoshi, Kai, Hiroyuki

“…[Display omitted] Selective N-methyl-d-aspartate receptor subunit 2B (NR2B) antagonists show potential as analgesic drugs, and do not cause side effects…”
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Discovery of orally bioavailable cyclohexanol-based NR2B-selective NMDA receptor antagonists with analgesic activity utilizing a scaffold hopping approach by Anan, Kosuke, Masui, Moriyasu, Hara, Shinichiro, Ohara, Miho, Kume, Masaharu, Yamamoto, Shoichi, Shinohara, Shunji, Tsuji, Hiroki, Shimada, Shinji, Yagi, Shigenori, Hasebe, Nobuyoshi, Kai, Hiroyuki

“…[Display omitted] NR2B subunit containing N-methyl-d-aspartate (NMDA) receptor is an attractive target for chronic pain due to its involvement in disease…”
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Orally Active Cephalosporins. IV. Synthesis, Antibacterial Activity and Oral Absorption of 3-(1H-1, 2, 3-Triazol-4-yl)thiomethylthio-cephalosporins by KUME, Masaharu, KUBOTA, Tadatoshi, KIMURA, Yasuo, NAKASHIMIZU, Hiromu, MOTOKAWA, Kiyoshi

“…The synthesis, antibacterial activity and oral absorption of 3-(1H-1, 2, 3, -trazol-4-yl)thiomethylthio-3-cephem-4-carboxylic acids with various C-7 side…”
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Orally Active Cephalosporins. I. Synthesis and Structure-Activity Relationships of 7β-[2-(R)-Amino-2-phenylacetamido]-3-(1H-1, 2, 3-triazol-4-yl) alkylthiomethyl-3-cephem-4-carboxylic Acid and Related Compounds by KUME, Masaharu, KUBOTA, Tadatoshi, KIMURA, Yasuo, NAKASHIMIZU, Hiromu, MOTOKAWA, Kiyoshi

“…The synthesis, antibacterial activity and oral absorbability of 7β-[2-(R)-amino-2-phenylacetamido]-3-(1H-1, 2, 3-triazol-4-yl)…”
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Total Synthesis of Luzopeptins A−C by Boger, Dale L, Ledeboer, Mark W, Kume, Masaharu

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Novel Antibacterial Macrolides:  Synthesis of 15-Membered Diolides by Ohara, Takafumi, Kume, Masaharu, Narukawa, Yukitoshi, Motokawa, Kiyoshi, Uotani, Kouichi, Nakai, Hiroshi

“…Novel 15-membered macrolides possessing the dilactone skeleton, diolides 13a and 13b, have been synthesized in our research program aimed at finding new…”
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Efficient and practical synthesis of 1⊝methylcarbapenems by Kume, Masaharu, Ooka, Hiroaki, Ishitobi, Hiroyuki

“…An efficient and practical method of synthesizing 1β-methylcarbapenem, S-4661, was developed. (4 R)-4-[(1S)-1-Methylallyl]-2-azetidinone 2, prepared from…”
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Novel and efficient synthesis of 1β-methylcarbapenems utilizing cyclization of hypervalent iodonium ylides by Kume, Masaharu, Kubota, Tadatoshi, Iso, Yasuyoshi

“…lβ-Methylcarbapenems were efficiently synthesized utilizing acid- and rhodium(II)-catalyzed cyclization of iodonium ylide intermediates, which were easily…”
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Orally Active Cephalosporins(第1報)7β-[2-(R)-Amino-2-phenylacetamido]-3-(1H-1,2,3-triazol-4-yl)alkylthiomethyl-3-cephem-4-carboxylic Acid及びその関連化合物の合成並びに構造活性相関 by 粂, 昌治, 久保田, 忠俊, 木村, 靖雄, 中清水, 弘, 元川, 清司

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The 7α-methoxy substituent in cephem or oxacephem antibiotics enhances in vivo anti-Helicobacter felis activity in mice after oral administration by Kobayashi, Yoshinao, Doi, Masayoshi, Nagata, Hiroshi, Kubota, Tadatoshi, Kume, Masaharu, Murakami, Kazuhisa

“…The in vivo antibacterial activities of 7α-methoxy-cephems or 7α-methoxy-1-oxacephems and their demethoxy congeners after oral administration were compared in…”
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The 7 -methoxy substituent in cephem or oxacephem antibiotics enhances in vivo anti-Helicobacter felis activity in mice after oral administration by Kobayashi, Y., Doi, M., Nagata, H., Kubota, T., Kume, M., Murakami, K.

“…The in vivo antibacterial activities of 7[alpha]-methoxy-cephems or 7[alpha]-methoxy-1-oxacephems and their demethoxy congeners after oral administration were…”
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Totalsynthese von Chinoxapeptin A–C: Bestimmung der absoluten Konfiguration by Boger, Dale L., Ledeboer, Mark W., Kume, Masaharu, Jin, Qing

“…Die relative und die absolute Konfiguration der natürlich vorkommenden, wirksamen Inhibitoren der Reversen Transkriptase (RT) von HIV, Chinoxapeptin A und B (1…”
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Orally Active Cephalosporins. I. Synthesis and Structure-Activity Relationships of 7β-[2-(R)-Amino-2-phenylacetamido]-3-(1H-1, 2, 3-triazol-4-yl) alkylthiomethyl-3-cephem-4-carboxylic Acid and Related Compounds by KUME, Masaharu, KUBOTA, Tadatoshi, KIMURA, Yasuo, NAKASHIMIZU, Hiromu, MOTOKAWA, Kiyoshi

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Orally active cephalosporins. III. Synthesis and structure-activity relationships of new 3-heterocyclicthiomethylthio-7 beta-[(Z)- 2-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamido]-3-cephem-4 -carboxylic acids by Kume, M, Kubota, T, Kimura, Y, Nakashimizu, H, Motokawa, K

“…3-Heterocyclicthiomethylthio-7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2- hydroxyiminoacetamido]-3-cephem-4-carboxylic acids (2) were synthesized. Their…”
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Totalsynthese von Chinoxapeptin A-C: Bestimmung der absoluten Konfiguration by Boger, Dale L., Ledeboer, Mark W., Kume, Masaharu, Jin, Qing

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