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Articles by Aoi Kimishima
A convergent total synthesis of the ivermectin aglycon through transition metal-mediated and anionic transformations
Abstract For decades, the avermectin class of macrolide natural products have played a critical role in the treatment of numerous infectious diseases and pests across the globe. Due to their biological activity and complex architecture, these natural products have inspired a great number of influential syntheses. Herein, we report a convergent total synthesis of the ivermectin B1a aglycon that addresses long‑standing challenges in constructing its highly functionalized macrolide framework.
Toward Combating Pseudomonas aeruginosa Infection, the Creation of Azithromycin Derivatives Based on a Trojan Horse Strategy
1 Introduction Antimicrobial resistance (AMR) is an ever-growing global problem, representing an evolutionary arms race between humanity’s innovations and rapidly adapting microbial defenses. Comprehensive estimates reveal that bacterial AMR directly caused 1.27 million deaths and contributed to 4.95 million deaths globally in 2019 [1]. By 2050, it is predicted that the number of deaths could reach 10 million unless actions are made to control AMR.
Binding Mode Based Chemical Screening Method Utilizing D-Ala-D-Ala Silica Gel Facilitating the Discovery of Overlooked Binding Affinity and Antibacterial Activity
1 Introduction Toward the development of new drug candidates, natural resources such as secondary metabolites produced by microorganisms and plant extracts have been attractive assets. Indeed, more than 56% of all small molecule drugs approved by the United States Food and Drug Administration (FDA) from 1981 to 2019 are natural products, compounds derived from natural products, or synthetic compounds inspired by natural products (Newman and Cragg 2020).
Atromentin B, Obtained by Microbial Fermentation and Total Synthesis, Potentiates the Activity of β-Lactams Against Methicillin-Resistant Staphylococcus aureus
Journal of Natural Products Cite this: J. Nat. Prod. 2025, XXXX, XXX Click to copy citationCitation copied! Learn about these metrics Article Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days. Citations are the number of other articles citing this article, calculated by Crossref and updated daily.
Efflux pump inhibitor, phenylalanine-arginine beta-naphthylamide analog potentiates the activity of 5-O-mycaminosyltylonolide for multi-drug resistant Pseudomonas aeruginosa | The Journal of Antibiotics
Abstract 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 resistance to many antibiotics due to the impermeability of its outer membrane and its multidrug efflux pump systems. Therefore, therapeutic drugs are limited, and the development of new drugs is extremely challenging.
A new tetronomycin analog, broad‐spectrum and potent antibiotic against drug‐resistant Gram‐positive bacteria
We discovered a new tetronomycin analog, C-32-OH tetronomycin (2) from the Streptomyces sp. K20-0247 strain, which produces tetronomycin (1). After NMR analysis of 2, we determined the planar structure. Futhermore, the absolute stereochemistry of 2 was deduced based on the biosynthetic pathway of 1 in the K20-0247 strain and a comparison of experimental electronic circular dichroism (ECD) results of 1 with 2.
The potentiation activity of β-lactam by phomoidrides and oxasetin against methicillin-resistant Staphylococcus aureus - The Journal of Antibiotics
Abstract 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 as meropenem (MEPM) is problematic. Therefore, we focus on combination drug therapy and have been seeking new potentiators of MEPM to combat MRSA.
Total Synthesis of Fusaramin, Enabling Stereochemical Elucidation, Structure-Activity Relationship, and Uncovering the Hidden Antimicrobial Activity against Plant Pathogenic Fungi | Organic Letters
Fusaramin (1) was isolated as a mitochondrial inhibitor. However, the fungal producer stops producing 1, which necessitates us to supply 1 by total synthesis. We proposed the complete stereochemical structure based on the biosynthetic pathway of sambutoxin. We have established concise and robust total synthesis of 1, enabling us to determine the complete stereochemical structure and to elucidate the structure–activity relationship, and uncover the hidden antiplant pathogenic fungal activity.
Emblestatin: a new peptide antibiotic from Embleya scabrispora K20-0267 - The Journal of Antibiotics
Abstract A new peptide, emblestatin (1), was discovered from a culture broth of Embleya scabrispora K20-0267. This strain was isolated from soil using an agar medium containing lysozyme. Based on NMR and mass spectrometric analyses, 1 consists of 2-(2-hydroxyphenyl)-2-oxazoline, β-alanine, glutamine, Nα-methyl-Nω-hydroxyornithine and 3-amino-1-hydroxy-2-piperidone moieties.
Comprehensive analysis of biosynthetic gene clusters in bacteria and discovery of Tumebacillus as a potential producer of natural products - The Journal of Antibiotics
Abstract Limited microbial genera such as Streptomyces have served as sources of natural products (NPs), whereas most others have been less investigated.
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