Search Results - "Inagaki, Hiroaki"
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Two distinct EF-Tu epitopes induce immune responses in rice and Arabidopsis
Published in Molecular plant-microbe interactions (01-02-2014)“…Plants sense potential pathogens by recognizing conserved pathogen-associated molecular patterns (PAMPs) that cause PAMP-triggered immunity (PTI). We…”
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Discovery of Novel 7-[(1R,5S)-1-Amino-5-fluoro-3-azabicyclo[3.3.0]octan-3-yl]-6-fluoro-1-[(1R,2S)-2-fluorocyclopropane]-8-(methoxy or methyl)quinolones
Published in Chemical & pharmaceutical bulletin (01-01-2019)“…A series of 8-methoxy or 8-methylquinolones bearing novel 3-aminooctahydrocyclopenta[c]pyrrole derivatives at the C-7 position was synthesized, and the…”
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Novel Peptidomimetics of the Antifungal Cyclic Peptide Rhodopeptin: Design of Mimetics Utilizing Scaffolding Methodology
Published in Organic letters (01-11-2001)“…Novel nonpeptide peptidomimetics of the antifungal cyclic peptide Rhodopeptin were designed utilizing hydantoin, benzimidazole, d-glucosamine, quinolone, and…”
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Design, Synthesis, and Biological Evaluation of Novel 7‑[(3aS,7aS)‑3a‑Aminohexahydropyrano[3,4‑c]pyrrol-2(3H)‑yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens
Published in Journal of medicinal chemistry (23-08-2018)“…Novel 7-[(3aS,7aS)-3a-aminohexahydropyrano[3,4-c]pyrrol-2(3H)-yl]-6-fluoro-1-[(1R,2S)-2-…”
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Practical Synthesis of DQ-113, a New Quinolone Antibacterial Agent, by Using the Intramolecular Horner-Wadsworth- Emmons Reaction
Published in Heterocycles (01-03-2004)Get full text
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Optimization of Novel Pyrido-pyridazinone Derivatives as FER Tyrosine Kinase Inhibitors, Leading to the Potent DS08701581
Published in ACS medicinal chemistry letters (11-07-2024)“…Previously, we reported the new pyrido-pyridazinone template as a feline sarcoma-related (FER) tyrosine kinase inhibitor. Representative compound 1…”
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Uterine leiomyosarcomas harboring MAP2K4 gene amplification are sensitive in vivo to PLX8725, a novel MAP2K4 inhibitor
Published in Gynecologic oncology (01-05-2023)“…Uterine leiomyosarcomas (uLMS) are rare, highly aggressive tumors. Up to 30% of uLMS may harbor gain of function (GOF) in the MAP2K4 gene, important for tumor…”
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Design, Synthesis, and Biological Evaluations of Novel 7‑[7-Amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens
Published in Journal of medicinal chemistry (14-03-2013)“…Novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-6-fluoro-1-[(1R,2S)-2-fluorocyclopropyl]- 8-methoxy-1,4-dihydro-4-oxoquinoline-3-carboxylic acid 2a and…”
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Discovery of Novel Pyrido-pyridazinone Derivatives as FER Tyrosine Kinase Inhibitors with Antitumor Activity
Published in ACS medicinal chemistry letters (09-05-2019)“…To obtain a new anticancer drug, we focused on FER tyrosine kinase. Starting with high-throughput screening with our in-house chemical library, compound 1,…”
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Improved synthesis of DQ-113, a new quinolone antibacterial agent, utilizing the Reformatsky reaction
Published in ARKIVOC (30-07-2003)Get full text
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Abstract B173: Preclinical characterization and antitumor efficacy of DS-5010, a highly potent and selective RET inhibitor
Published in Molecular cancer therapeutics (01-01-2018)“…Abstract Background: RET gene rearrangement has been detected in several cancers including 1-2% and 50% of non-small cell lung cancer (NSCLC) and papillary…”
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Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria
Published in Bioorganic & medicinal chemistry (01-10-2009)“…A series of novel 6-desfluoro [des-F(6)] and 6-fluoro-1-[(1 R,2 S)-2-fluorocyclopropan-1-yl]-8-methoxyquinolones bearing 3-(1-aminocycloalkyl)pyrrolidin-1-yl…”
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Characterization and Optimization of Selective, Nonpeptidic Inhibitors of Cathepsin S with an Unprecedented Binding Mode
Published in Journal of medicinal chemistry (31-05-2007)“…The substrate activity screening (SAS) method, a substrate-based fragment identification and optimization method for the development of enzyme inhibitors, was…”
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Synthesis and Antifungal Activity of Rhodopeptin Analogues. 2. Modification of the West Amino Acid Moiety
Published in Organic letters (06-04-2000)“…Structure−activity relationships of the west amino acid modified analogues of rhodopeptins, novel antifungal tetrapeptide isolated from Rhodococcus species…”
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Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position
Published in Bioorganic & medicinal chemistry letters (18-10-2004)“…New quinolone compounds were synthesized and evaluated their antibacterial activity and enzyme selectivity. A series of novel…”
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Synthesis and Structure−Activity Relationships of 5-Amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic Acid Antibacterials Having Fluorinated 7-[(3R)-3-(1-Aminocyclopropan-1-yl)pyrrolidin-1-yl] Substituents
Published in Journal of medicinal chemistry (13-03-2003)“…A series of novel 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolones bearing fluorinated (3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl…”
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Novel Peptidomimetics of the Antifungal Cyclic Peptide Rhodopeptin: Synthesis of Mimetics and Their Antifungal Activity
Published in Organic letters (01-11-2001)“…Novel peptidomimetics of the antifungal cyclic peptide Rhodopeptin were synthesized. As with the cyclic peptides, the presence of all three Rhodopeptin side…”
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Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R, 2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxyli c acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents
Published in Journal of medicinal chemistry (2003)Get full text
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Synthesis and Antifungal Activity of Rhodopeptin Analogues. 1. Modification of the East and South Amino Acid Moieties
Published in Organic letters (06-04-2000)“…Structure−activity relationships of the east and south amino acid modified analogues of rhodopeptins, novel antifungal cyclic tetrapeptides isolated from…”
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