A5078878264- Microbial Natural Products and Biosynthesis
- Synthetic Organic Chemistry Methods
- Carbohydrate Chemistry and Synthesis
- Chemical Synthesis and Analysis
- Chemical synthesis and alkaloids
- Plant biochemistry and biosynthesis
- Click Chemistry and Applications
- Studies on Chitinases and Chitosanases
- Asymmetric Synthesis and Catalysis
- Marine Sponges and Natural Products
- Traditional and Medicinal Uses of Annonaceae
- Alkaloids: synthesis and pharmacology
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Bioactive Compounds and Antitumor Agents
- Antibiotic Resistance in Bacteria
- Synthesis and Biological Evaluation
- Enzyme Production and Characterization
- Peptidase Inhibition and Analysis
- Fungal Biology and Applications
- Antimicrobial Peptides and Activities
- Cholesterol and Lipid Metabolism
- Natural product bioactivities and synthesis
- Steroid Chemistry and Biochemistry
- Oxidative Organic Chemistry Reactions
Kitasato University
2016-2025
Kitasato Institute Hospital
2014-2024
Japan Science and Technology Agency
2006
The University of Tokyo
2000
Bayer (Germany)
2000
Fuji Chemical Industries (Japan)
1994-1997
Pfizer (Japan)
1996
Daiichi Sankyo (Germany)
1994
Daiichi-Sankyo (South Korea)
1994
Philadelphia University
1991
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTMacrolides with gastrointestinal motor stimulating activitySatoshi Omura, Kazuo Tsuzuki, Toshiaki Sunazuka, Shogo Marui, Hajime Toyoda, Nobuhiro Inatomi, and Zen ItohCite this: J. Med. Chem. 1987, 30, 11, 1941–1943Publication Date (Print):November 1, 1987Publication History Published online1 May 2002Published inissue 1 November 1987https://pubs.acs.org/doi/10.1021/jm00394a001https://doi.org/10.1021/jm00394a001research-articleACS PublicationsRequest...
ADVERTISEMENT RETURN TO ISSUEPREVCommunicationNEXTTotal Synthesis of (+)-Madindoline A and (−)-Madindoline B, Potent, Selective Inhibitors Interleukin 6. Determination the Relative Absolute ConfigurationsToshiaki Sunazuka, Tomoyasu Hirose, Tatsuya Shirahata, Yoshihiro Harigaya, Masahiko Hayashi, Kanki Komiyama, Satoshi Ōmura, Amos B. SmithView Author Information Research Center for Biological Function The Kitasato Institute School Pharmaceutical Sciences University, Minato-ku, Tokyo 108,...
Afidopyropen, a novel insecticide, is derivative of pyripyropene A, which produced by the filamentous fungus Penicillium coprobium. Afidopyropen has strong insecticidal activity against aphids and currently used as control agent sucking pests worldwide. In this study, we summarized biological properties field efficacies its derivatives agricultural using official trials conducted in Japan. showed good residual variety aphids, whiteflies other under conditions. Furthermore, toxicological...
Infections with parasitic helminths are important causes of morbidity and mortality worldwide. New drugs that parasite specific minimally toxic to the host needed counter these infections effectively. Here we report finding a previously unidentified compound, nafuredin, from Aspergillus niger . Nafuredin inhibits NADH-fumarate reductase (complexes I + II) activity, unique anaerobic electron transport system in helminth mitochondria, at nM order. It competes for quinone-binding site complex...
Long-term macrolide therapy has been proven to improve survival in patients with diffuse panbronchiolitis. Although its mechanisms remain unknown, previous studies have suggested the effects of might be anti-inflammatory rather than antibacterial. To elucidate molecular action, we studied here erythromycin (EM) and new derivative, EM703, which shows no antibacterial on activation transcription factor nuclear factor-kappaB (NF-kappaB) human bronchial epithelial cells. Western blotting...
Chemical modifications of 8,9-anhydroerythromycin A 6,9-hemiacetal (1), which showed gastrointestinal motor stimulating (GMS) activity 10 times more potent than that erythromycin (EM-A), were undertaken to search for derivatives having stronger GMS and no antimicrobial activity; details are described in this a subsequent paper. Displacement methyl group the dimethylamino 1 with an ethyl isopropyl provided de(N-methyl-N-ethyl-8,9-anhydroerythromycin (55)...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTTotal synthesis of (+)-lactacystin, the first non-protein neurotrophic factorToshiaki Sunazuka, Tohru Nagamitsu, Keiichi Matsuzaki, Haruo Tanaka, Satoshi Omura, and Amos B. Smith IIICite this: J. Am. Chem. Soc. 1993, 115, 12, 5302Publication Date (Print):June 1, 1993Publication History Published online1 May 2002Published inissue 1 June 1993https://pubs.acs.org/doi/10.1021/ja00065a054https://doi.org/10.1021/ja00065a054research-articleACS...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTRelative and Absolute Stereochemistry of Pyripyropene A, A Potent, Bioavailable Inhibitor Acyl-CoA:Cholesterol Acyltransferase (ACAT)Hiroshi Tomoda, Hiroyuki Nishida, Young Kook Kim, Rika Obata, Toshiaki Sunazuka, Satoshi Omura, Jon Bordner, Mark Guadliana, Peter G. Dormer, Amos B. Smith IIICite this: J. Am. Chem. Soc. 1994, 116, 26, 12097–12098Publication Date (Print):December 1, 1994Publication History Published online1 May 2002Published inissue...
Supported total synthesis: The combinatorial synthesis of a 122-membered macrosphelide library including macrosphelides A, C, E, and F (see picture) has been achieved based on unique strategy for three-component coupling utilizing palladium-catalyzed chemoselective carbonylation an unprecedented macrolactonization polymer support. Supporting information this article is available the WWW under http://www.wiley-vch.de/contents/jc_2002/2003/z52229_s.pdf or from author. Please note: publisher...
After 50 years of persistence the 12-membered cyclic skeleton bottromycin A2 (3) has been confirmed by NMR experiments (HMBC), and configurations two tLeu residues have estimated conformation analysis experiments. Furthermore, key step in synthesis 3 involves mercury-mediated formation amidine thioamide 1 amine 2. Detailed facts importance to specialist readers are published as "Supporting Information". Such documents peer-reviewed, but not copy-edited or typeset. They made available...
Pancreatic cancer is one of the most difficult types to treat because its high mortality rate due chemotherapy resistance. We previously reported that combined treatment with gefitinib (GEF) and clarithromycin (CAM) results in enhanced cytotoxicity GEF along endoplasmic reticulum (ER) stress loading non-small cell lung lines. An epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) such as induces autophagy a pro-survival role, whereas CAM inhibits flux various Pronounced...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTTotal Synthesis of (+)-Pyripyropene A, a Potent, Orally Bioavailable Inhibitor Acyl-CoA:Cholesterol AcyltransferaseTohru Nagamitsu, Toshiaki Sunazuka, Rika Obata, Hiroshi Tomoda, Haruo Tanaka, Yoshihiro Harigaya, Satoshi Omura, and Amos B. Smith IIICite this: J. Org. Chem. 1995, 60, 25, 8126–8127Publication Date (Print):December 1, 1995Publication History Published online1 May 2002Published inissue 1 December...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTTotal syntheses of (+)-paspalicine and (+)-paspalinineAmos B. Smith III, Toshiaki Sunazuka, Tamara L. Leenay, Jill Kingery-WoodCite this: J. Am. Chem. Soc. 1990, 112, 22, 8197–8198Publication Date (Print):October 1, 1990Publication History Published online1 May 2002Published inissue 1 October 1990https://pubs.acs.org/doi/10.1021/ja00178a071https://doi.org/10.1021/ja00178a071research-articleACS PublicationsRequest reuse permissionsArticle...
Bioactive natural products produced by microbes have almost limitless potential in pharmaceutical applications, and the organic synthesis of such as lead compounds will result creation new widely useful products. A program discovery naturally occurring bioactive microbial metabolites has been ongoing at Kitasato Institute. We also developed efficient, rational, highly flexible production methods for generation target compounds, related elucidation their structure-activity relationships,...
A first asymmetric total synthesis and determination of the absolute configuration neoxaline has been accomplished through highly stereoselective introduction a reverse prenyl group to create quaternary carbon stereocenter using (-)-3a-hydroxyfuroindoline as building block, construction indoline spiroaminal via cautious stepwise oxidations with cyclizations from indoline, assembly (Z)-dehydrohistidine, photoisomerization unnatural (Z)-neoxaline natural (E)-neoxaline key steps.