The activities of telithromycin and levofloxacin against 99 mycoplasma strains were compared to those of several macrolides, ofloxacin, and doxycycline. Telithromycin MICs of
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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 PDFSynthesis and structure-activity relationships of novel 14-membered 2-fluoro ketolides with structural modification at the C11 position.
Eur J Med Chem
March 2024
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, No.1 TiantanXili, Beijing 100050, China. Electronic address:
A series of novel C11 substituted 14-membered 2-fluoro ketolides were synthesized and evaluated for their antibacterial activity against erythromycin-resistant and erythromycin-susceptible clinical isolates and strains from ATCC. The overall antibacterial spectra of the semi-synthetic antibiotics are similar to that of telithromycin (TEL) and most of them exhibited excellent activity against Gram-positive bacteria (S. epidermidis, S.
View Article and Find Full Text PDFPythium insidiosum: In vitro oomicidal evaluation of telithromycin and interactions with azithromycin and amorolfine hydrochloride.
J Mycol Med
March 2024
Departamento de Medicina Veterinária Preventiva, Laboratório de Saúde Única, Programa de Pós-graduação em Ciências Farmacêuticas (PPGCF) e de Medicina Veterinária (PPGMV), Centro de Ciências Rurais, Universidade Federal de Santa Maria (UFSM), Av. Roraima N° 1000, Prédio 44, sala 5132, CEP, Santa Maria, RS 97105-900, Brazil. Electronic address:
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