A set of 4-quinolone-3-carboxylic acids bearing different substituents on the condensed benzene ring was designed and synthesized as potential HIV-1 integrase inhibitors structurally related to elvitegravir. Some of the new compounds proved to be able to inhibit the strand transfer step of the virus integration process in the micromolar range. Docking studies and quantum mechanics calculations were used to rationalize these data.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/jm8003784 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Update on HIV Chemoprevention.
Annu Rev Med
January 2025
University of California, Los Angeles (UCLA) Clinical AIDS Research and Education (CARE) Center, Department of Medicine, David Geffen School of Medicine at UCLA, Los Angeles, California, USA; email:
Despite rapid advances in the field of HIV prevention and treatment, unacceptably high global HIV incidence rates highlight the ongoing need for effective HIV prevention interventions for populations at risk for HIV acquisition. This article provides an updated review of the current data surrounding HIV prevention strategies, including treatment as prevention (TasP), preexposure prophylaxis (PrEP), and postexposure prophylaxis (PEP), as well as advances in sexually transmitted infection biomedical prevention. This review provides an overview of the multiple PrEP modalities that are available globally, such as oral PrEP, injectable cabotegravir, and the dapivirine vaginal ring, and describes their respective clinical trials, efficacies, and regulatory approvals.
View Article and Find Full Text PDFPretreatment HIV Drug Resistance to Integrase Strand Transfer Inhibitors Among Newly Diagnosed HIV Individuals - China, 2018-2023.
China CDC Wkly
January 2025
State Key Laboratory of Infectious Disease Prevention and Control, National Center for AIDS/STD Control and Prevention, Chinese Center for Disease Control and Prevention, Beijing, China.
Introduction: The widespread adoption of integrase strand transfer inhibitors (INSTIs) has led to the emergence of INSTI-associated drug-resistance mutations. This cross-sectional study conducted a comprehensive national survey to investigate the prevalence of pretreatment drug resistance (PDR) to INSTIs among newly diagnosed human immunodeficiency virus (HIV) individuals in China.
Methods: The study enrolled 10,654 individuals from 31 provincial-level administrative divisions between 2018 and 2023.
Transmitted HIV-1 Drug Resistance in Estonian Residents and Ukrainian Refugees in 2020 and 2022.
J Glob Antimicrob Resist
January 2025
Faculty of Medicine, Department of Microbiology, University of Tartu, Tartu, Estonia.
Objectives: We investigated the prevalence of drug resistance mutations (DRMs) in individuals newly diagnosed with HIV-1 in Estonia in 2020 and 2022, and in Ukrainian war refugees living with HIV who arrived in Estonia in 2022.
Methods: HIV-1 genomic RNA was sequenced in protease-reverse transcriptase and integrase regions. DRMs were determined separately by Stanford University CPR Tool and HIVdb Program.
Comparative Analyses of Antiviral Potencies of Second-Generation Integrase Strand Transfer Inhibitors (INSTIs) and the Developmental Compound 4d Against a Panel of Integrase Quadruple Mutants.
Viruses
January 2025
Chemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Frederick, MD 21702, USA.
Second-generation integrase strand transfer inhibitors (INSTIs) are strongly recommended for people living with HIV-1 (PLWH). The emergence of resistance to second-generation INSTIs has been infrequent and has not yet been a major issue in high-income countries. However, the delayed rollouts of these INSTIs in low- to middle-income countries during the COVID-19 pandemic combined with increased transmission of drug-resistant mutants worldwide are leading to an increase in INSTI resistance.
View Article and Find Full Text PDFDrug-Drug Interactions Between HIV Antivirals and Concomitant Drugs in HIV Patients: What We Know and What We Need to Know.
Pharmaceutics
December 2024
Clinical Pharmacology Unit, San Giovanni di Dio e Ruggi d'Aragona University Hospital, 84131 Salerno, Italy.
Highly active antiretroviral therapy has led to a significant increase in the life expectancy of people living with HIV. The trade-off is that HIV-infected patients often suffer from comorbidities that require additional treatment, increasing the risk of Drug-Drug Interactions (DDIs), the clinical relevance of which has often not been determined during registration trials of the drugs involved. Therefore, it is important to identify potential clinically relevant DDIs in order to establish the most appropriate therapeutic approaches.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!