Search Results - "Masaki Tomishima"
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Fragment-Based Discovery of Pyrimido[1,2-b]indazole PDE10A Inhibitors
Published in Chemical & pharmaceutical bulletin (2018)“…In this study, we report the identification of potent pyrimidoindazoles as phosphodiesterase10A (PDE10A) inhibitors by using the method of fragment-based drug…”
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2
Total Synthesis of Chloropeptin II (Complestatin) and Chloropeptin I
Published in Journal of the American Chemical Society (11-11-2009)“…The first total synthesis of chloropeptin II (1, complestatin) is disclosed. Key elements of the approach include the use of an intramolecular Larock indole…”
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3
Novel echinocandin antifungals. Part 2: Optimization of the side chain of the natural product FR901379. Discovery of micafungin
Published in Bioorganic & medicinal chemistry (01-05-2008)“…Further optimization of the potent antifungal activity of side chain analogs of the natural product FR901379 led to the discovery of compound 8 (micafungin)…”
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In Vitro Activities of a New Lipopeptide Antifungal Agent, FK463, against a Variety of Clinically Important Fungi
Published in Antimicrobial Agents and Chemotherapy (01-01-2000)“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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5
Novel echinocandin antifungals. Part 1: Novel side-chain analogs of the natural product FR901379
Published in Bioorganic & medicinal chemistry (15-02-2008)“…A series of novel acylated analogs of the novel water-soluble echinocandin FR901379 have been prepared. Compound 3c shows both potent antifungal activity and…”
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6
Use of a serum-based antifungal susceptibility assay to predict the in vivo efficacy of novel echinocandin compounds
Published in Microbiology and immunology (01-08-2008)“…ABSTRACT In vitro susceptibility assays of antifungal activity do not always accurately predict in vivo efficacy. As well as having a clear clinical…”
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FK463, a novel water-soluble echinocandin lipopeptide: synthesis and antifungal activity
Published in Journal of antibiotics (1999)Get more information
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8
Determination of Antifungal Activities in Serum Samples from Mice Treated with Different Antifungal Drugs Allows Detection of an Active Metabolite of Itraconazole
Published in Microbiology and immunology (2006)“…To establish an in vitro method of predicting in vivo efficacy of antifungal drugs against Candida albicans and Aspergillus fumigatus, the antifungal…”
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Novel benzimidazole derivatives as phosphodiesterase 10A (PDE10A) inhibitors with improved metabolic stability
Published in Bioorganic & medicinal chemistry (01-07-2014)“…In this study, we report the identification of potent benzimidazoles as PDE10A inhibitors. We first identified imidazopyridine 1 as a high-throughput screening…”
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10
Synthesis, SAR study, and biological evaluation of novel 2,3-dihydro-1H-imidazo[1,2-a]benzimidazole derivatives as phosphodiesterase 10A inhibitors
Published in Bioorganic & medicinal chemistry (15-08-2019)“…[Display omitted] Phosphodiesterase 10A (PDE10A) inhibitors were designed and synthesized based on the dihydro-imidazobenzimidazole scaffold. Compound 5a…”
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11
Fragment-Based Discovery of Pyrimido[1,2-b]indazole PDE10A Inhibitors
Published in Chemical and Pharmaceutical Bulletin (01-03-2018)“…In this study, we report the identification of potent pyrimidoindazoles as phosphodiesterase10A (PDE10A) inhibitors by using the method of fragment-based drug…”
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12
Synthesis and antifungal activity of ASP9726, a novel echinocandin with potent Aspergillus hyphal growth inhibition
Published in Bioorganic & medicinal chemistry letters (15-02-2014)“…The synthesis and antifungal activity of ASP9726, a novel echinocandin with potent Aspergillus hyphal growth inhibition and significantly improved MIC against…”
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13
FR290581, a novel sordarin derivative: Synthesis and antifungal activity
Published in Bioorganic & medicinal chemistry letters (01-03-2009)“…We have discovered the novel sordarin derivative FR290581, which exhibited superior activity, a good pharmacokinetic profile and good in vivo activity…”
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14
Synthesis and evaluation of nitro 5-deazaflavins as novel bioreductive antitumor agents
Published in Bioorganic & medicinal chemistry letters (21-09-1995)“…A series of nitro 5-deazaflavins, 5-deazaflavins possessing a nitro group at C(6)–C(9) position, has been designed and synthesized as a novel class of…”
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Atropisomeric Flavoenzyme Models with a Modified Pyrimidine Ring: Syntheses, Physical Properties, and Stereochemistry in the Reactions with NAD(P)H Analogs
Published in Journal of organic chemistry (27-12-1996)“…Optically active 5-deazaflavin derivatives (3-aryl-10-(4-tert-butylphenyl)pyrimido[4,5-b]quinoline-2,4(3H,10H)-dione) with an axial chirality at the pyrimidine…”
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Evaluation of differential hypoxic cytotoxicity and electrochemical studies of nitro 5-deazaflavins
Published in Bioorganic & medicinal chemistry letters (21-09-1995)“…Cytotoxicities of nitro 5-deazaflavins were evaluated in vitro towards hypoxic and oxic Chinese hamster cells (V79). 6-Nitro and 8-nitro derivatives were…”
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