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Repurposing zidovudine and 5-fluoro-2'-deoxyuridine as antibiotic drugs made possible by synergy with both trimethoprim and the mitochondrial toxicity-reducing agent uridine.
J Antimicrob Chemother
December 2024
Ultupharma AB, Södra Rudbecksgatan 13, Uppsala SE-752 36, Sweden.
Objectives: The increasing frequency of antibiotic-resistant bacterial infections is a major public health challenge, and new antibiotic drugs are urgently needed. A rapid solution to the problem is to repurpose clinically approved compounds with antibacterial properties, such as the nucleoside analogues zidovudine (azidothymidine) or 5-fluoro-2'-deoxyuridine. Here we report the in vitro and in vivo antibacterial properties of double and triple combinations of azidothymidine or 5-fluoro-2'-deoxyuridine with uridine and/or trimethoprim.
View Article and Find Full Text PDFSynthesis of β-lactam-zidovudine pronucleosides as potential selective narrow-spectrum antibacterial agents.
Org Biomol Chem
January 2025
Institut des Biomolécules Max Mousseron, Univ Montpellier, CNRS, ENSCM, Montpellier, France.
Since the discovery of penicillin, the forerunner of the most widely used class of antibiotics ( β-lactams), natural compounds and their derivatives represented a major source of antibacterial therapeutic products whose availability enabled modern medical practices (invasive surgery, organ transplant, .). However, the relentless emergence of resistant bacteria is challenging the long-term efficacy of antibiotics, also decreasing their economic attractiveness for big pharma, leading to a significant decay in antibacterial development in the 21 century and an increased use of last-resort drugs such as carbapenems or colistin.
View Article and Find Full Text PDFDesign, , and Evaluation of Polymer-Based Drug Conjugates Incorporated with Derivative of Cinnamic Acid, Zidovudine, and 4-Aminosalicylic Acid against Pseudo-HIV-1.
Curr HIV Res
January 2025
Department of Chemistry, University of Fort Hare, Alice, South Africa.
Article Synopsis
- The study explores the use of polymer-drug conjugates to enhance the efficacy of zidovudine, an anti-HIV drug, both alone and with other drugs.
- Researchers prepared these conjugates using a specific polymerization method and analyzed their characteristics and potential.
- Results indicated that some conjugates showed strong effectiveness against pseudo-HIV-1, highlighting their promise as future anti-HIV treatments that warrant further investigation.
Screening miRNAs to Hinder the Tumorigenesis of Renal Clear Cell Carcinoma Associated with KDR Expression.
Curr Cancer Drug Targets
September 2024
Centre for Bioinformatics, Department of Biochemistry, Karpagam Academy of Higher Education, Coimbatore, Tamil Nadu, 641021, India.
Article Synopsis
- The study investigates the role of Kinase Insert Domain Receptor (KDR) and its associated microRNAs (miRNAs) in renal cell carcinoma, highlighting the potential importance of their findings for future research.
- Utilizing various databases and tools, the researchers identified how miRNAs regulate KDR expression and validated their results with patient samples.
- Results showed that KDR expression was significantly elevated in tumor tissues compared to normal tissues, with miR-200c-3p being notably down-regulated, suggesting that higher levels of this miRNA could reduce KDR expression and potentially inhibit cancer progression.
Characterizing HIV drug resistance in cases of vertical transmission in the VESTED randomized antiretroviral treatment trial.
J Acquir Immune Defic Syndr
August 2024
Department of Global Infectious Diseases, Seattle Children's Research Institute, 307 Westlake Ave N, Seattle, 98109, Washington, USA.
Article Synopsis
- - VESTED (NCT03048422) compared the safety and effectiveness of three antiretroviral therapy regimens in pregnant and postpartum women with HIV, finding a low vertical transmission rate of 0.60% among infants.
- - The study analyzed data from 2018 to 2020, enrolling women in early pregnancy and measuring outcomes up to 50 weeks postpartum, focusing on HIV drug resistance in cases of transmission.
- - Results revealed that mothers taking efavirenz-based treatment prior to switching to dolutegravir likely contributed to the transmission of specific HIV drug resistance mutations to their infants, despite prophylactic treatment.
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