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Thiazoplanomicin, a new thiazolyl peptide antibiotic from the leaf-litter actinomycete Actinoplanes sp. MM794L-181F6.
J Antibiot (Tokyo)
January 2025
Institute of Microbial Chemistry (BIKAKEN), Shinagawa-ku, Tokyo, Japan.
A new bioactive substance was identified from a leaf-litter actinomycete strain by screening for antibacterial activity against Neisseria gonorrhoeae. The thiazolyl peptide antibiotic, named thiazoplanomicin, was isolated from the secondary metabolites of the leaf-litter actinomycetes Actinoplanes sp. MM794L-181F6 by extraction with n-butanol, silica gel column chromatography, Sephadex LH-20 column chromatography, and preparative HPLC.
View Article and Find Full Text PDFIdentification of novel anti-leishmanials targeting glutathione synthetase of the parasite: a drug repurposing approach.
FEBS Lett
September 2024
School of Biochemical Engineering, Indian Institute of Technology (BHU), Varanasi, India.
Drug repurposing has emerged as an effective strategy against infectious diseases such as visceral leishmaniasis. Here, we evaluated four FDA-approved drugs-valrubicin, ciclesonide, deflazacort, and telithromycin-for their anti-leishmanial activity on Leishmania donovani parasites, especially their ability to target the enzyme glutathione synthetase (LdGS), which enables parasite survival under oxidative stress in host macrophages. Valrubicin and ciclesonide exhibited superior inhibitory effects compared to deflazacort and telithromycin, inhibiting the promastigotes at very low concentrations, with IC values of 1.
View Article and Find Full Text PDFSynthetic macrolides overcoming MLSK-resistant pathogens.
Cell Discov
July 2024
Key Laboratory of Medicinal Molecule Science and Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, Beijing Institute of Technology, Beijing, China.
Conventional macrolide-lincosamide-streptogramin B-ketolide (MLSK) antibiotics are unable to counter the growing challenge of antibiotic resistance that is conferred by the constitutive methylation of rRNA base A2058 or its G2058 mutation, while the presence of unmodified A2058 is crucial for high selectivity of traditional MLSK in targeting pathogens over human cells. The absence of effective modes of action reinforces the prevailing belief that constitutively antibiotic-resistant Staphylococcus aureus remains impervious to existing macrolides including telithromycin. Here, we report the design and synthesis of a novel series of macrolides, featuring the strategic fusion of ketolide and quinolone moieties.
View Article and Find Full Text PDFClinical characteristics and risk factors for poor outcomes of invasive pneumococcal disease in pediatric patients in China.
BMC Infect Dis
June 2024
Department of Pediatrics, Qilu Hospital of Shandong University, No.107 West Wenhua Road, Jinan, 250012, Shandong Province, China.
Background: Invasive pneumococcal disease (IPD) is a significant health concern in children worldwide. In this study, we aimed to analyze the clinical features, antibiotic resistance, and risk variables for poor outcomes in patients with IPD in Hangzhou.
Methods: A retrospective single-centre study was performed using the pediatric intensive care (PIC) database from 2010 to 2018.
Changes in the epidemiology and antimicrobial resistance patterns of Streptococcus pneumoniae from pediatric community acquired pneumonia patients attended in a Chinese hospital during the COVID-19 pandemic.
Infection
December 2024
Department of General Practice, Yongchuan Hospital of Chongqing Medical University, No. 439, Xuanhua Street, Chongqing, 402160, China.
Purpose: The COVID-19 pandemic has altered the infection dynamics of numerous pathogens. This study aimed to elucidate its impact on Streptococcus pneumoniae (S. pneumoniae) infections in children with community acquired pneumonia (CAP).
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