22 Result(s)
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Article
Hideaki Hanaki
Life Sciences, general
Microbiology
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Article
Efflux pump inhibitor, phenylalanine-arginine beta-naphthylamide analog potentiates the activity of 5-O-mycaminosyltylonolide for multi-drug resistant Pseudomonas aeruginosa
The emergence and spread of antimicrobial resistance are global threats. Pseudomonas aeruginosa (P. aeruginosa) is responsible for a substantial proportion of this global health issue because of its intrinsic res...
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Article
The potentiation activity of β-lactam by phomoidrides and oxasetin against methicillin-resistant Staphylococcus aureus
Antimicrobial resistance (AMR) causes a global health threat and enormous damage for humans. Among them, Methicillin-resistant Staphylococcus aureus (MRSA) resistant to first-line therapeutic β-lactam drugs such ...
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Article
Antifungal profile against Candida auris clinical isolates of tyroscherin and its new analog produced by the deep-sea-derived fungal strain Scedosporium apiospermum FKJ-0499
A new antifungal compound, named N-demethyltyroscherin (1), was discovered from the static fungal cultured material of Scedosporium apiospermum FKJ-0499 isolated from a deep-sea sediment sample together with a kn...
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Article
A novel aromatic compound from the fungus Synnemellisia sp. FKR-0921
The filamentous fungus Synnemellisia sp. strain FKR-0921 was obtained from soil collected on Kume Island, Okinawa. The MeOH extract of FKR-0921 cultured on a solid rice medium yielded a new aromatic compound, syn...
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Article
Open AccessProphylactic administration of ivermectin attenuates SARS-CoV-2 induced disease in a Syrian Hamster Model
COVID-19, caused by SARS-CoV-2 infection, is currently among the most important public health concerns worldwide. Although several effective vaccines have been developed, there is an urgent clinical need for e...
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Article
A combination strategy of a semisynthetic macrolide, 5-O-mycaminosyltylonolide with polymyxin B nonapeptide for multi-drug resistance P. aeruginosa
The emergence and spread of antimicrobial resistant pathogens continue to threaten our ability to combat several infections. Among them, Pseudomonas aeruginosa (P. aeruginosa) poses a major threat to human health...
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Article
An efflux pump deletion mutant enabling the discovery of a macrolide as an overlooked anti-P. aeruginosa active compound
Antimicrobial resistance is a serious, worldwide problem. Pseudomonas aeruginosa (P. aeruginosa) is the pathogen that poses a major threat to human health. However, resistance-nodulation-cell division type multid...
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Article
Landscape of blaNDM genes in Enterobacteriaceae
The blaNDM-1 gene encodes a carbapenemase, New Delhi metallo-β-lactamase (NDM-1), and the ability to produce NDM-1 is spread among Enterobacteriaceae via horizontal gene transfer of plasmids. It has been widely a...
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Article
Clonocoprogens A, B and C, new antimalarial coprogens from the Okinawan fungus Clonostachys compactiuscula FKR-0021
Three new antimalarial compounds, clonocoprogens A, B, and C, were isolated from the static culture of an Okinawan fungus, Clonostachys compactiuscula FKR-0021. These compounds were new analogs of N14-palmitoylco...
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Article
5-O-Mycaminosyltylonolide antibacterial derivatives: design, synthesis and bioactivity
Tylosin is a 16-membered macrolide broad-spectrum antibiotic that has an important role in veterinary medicine, active against Gram-positive and a restricted range of Gram-negative bacteria. We synthesized 15 ...
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Article
Total synthesis of (±)-naphthacemycin A9, possessing both antibacterial activity against methicillin-resistant Staphylococcus aureus and circumventing effect of β-lactam resistance
The total synthesis of KB-3346-5A9, named naphthacemycin A9, has been accomplished by combining the Dötz reaction and Suzuki–Miyaura cross coupling as well as employing Friedel–Crafts reaction with dienone-phenol...
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Article
Naphthacemycins, novel circumventors of β-lactam resistance in MRSA, produced by Streptomyces sp. KB-3346-5. I. The taxonomy of the producing strain, and the fermentation, isolation and antibacterial activities
Screening for circumventors of β-lactam resistance in methicillin-resistant Staphylococcus aureus (MRSA) led us to find 17 novel antibiotics, naphthacemycins A1–A11, B1–B4 and C1–C2. The naphthacemycins were isol...
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Article
Naphthacemycins, novel circumventors of β-lactam resistance in MRSA, produced by Streptomyces sp. KB-3346-5. II. Structure elucidation
Seventeen new compounds, naphthacemycins A1–A11, B1–B4 and C1–C2, were isolated from a cultured broth of Streptomyces sp. KB-3346-5 during screening for circumventors of β-lactam resistance in methicillin-resista...
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Article
Paraphaeosphaeride D and berkleasmin F, new circumventors of arbekacin resistance in MRSA, produced by Paraphaeosphaeria sp. TR-022
Two new compounds, designated paraphaeosphaeride D (1) and berkleasmin F (2) together with a previously known compound, berkleasmin A (3), isolated from a culture broth of the fungus Paraphaeosphaeria sp. TR-022,...
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Non-antibiotic 12-membered macrolides: design, synthesis and biological evaluation in a cigarette-smoking model
The 14-membered macrolide erythromycin A expresses three distinct biological properties, including antibacterial activity, gastrointestinal motor-stimulating activity and anti-inflammatory and/or immunomodulat...
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Antimalarial C-9 oxime derivatives from desmycosin, produced by click chemistry
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Aranorosin circumvents arbekacin-resistance in MRSA by inhibiting the bifunctional enzyme AAC(6′)/APH(2″)
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Open AccessLow level β-lactamase production in methicillin-resistant staphylococcus aureus strains with β-lactam antibiotics-induced vancomycin resistance
A class of methicillin-resistant Staphylococcus aureus (MRSA) shows resistance to vancomycin only in the presence of β-lactam antibiotics (BIVR). This type of vancomycin resistance is mainly attributable to the r...
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Identification of the active component that induces vancomycin resistance in MRSA
A fraction of methicillin-resistant Staphylococcus aureus (MRSA) shows resistance to vancomycin (VCM) in the presence of β-lactam antibiotics (BIVR) at low concentrations. We hypothesized that the BIVR phenomenon...
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4″′-N-Demethylspiramycin Derivatives: Synthesis and Evaluation of Effectiveness against Drug-resistant Bacteria
18-Amino-4″-O-benzoyl-4″′-N-demethyl-18-deoxospiramycins were designed and synthesized. Synthetic strategy involved selective demethylation of the dimethylamino group in forosamine, benzoylation of the hydroxyl g...
