ArticleJournal of medicinal chemistry2011
Design, synthesis, and biological evaluation of triazolo-pyrimidine derivatives as novel inhibitors of hepatitis B virus surface antigen (HBsAg) secretion.
Article in Journal of medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
27 citing papers in PubMed, 117 citations in OpenAlex.
- Synthesis, SAR, and in silico studies of new benzochromene derivatives as insecticidal agents against Culex pipiens L. larvae and adults.Scientific reports · 2025Article
- Synthesis, characterization and biological profile of some new dihydropyrimidinone derivaties.Heliyon · 2025Article
- Three-Component Synthesis of 1-Substituted 5-Aminotetrazoles Promoted by Bismuth Nitrate.The Journal of organic chemistry · 2024Article
- Novel Substituted Azoloazines with Anticoagulant Activity.International journal of molecular sciences · 2023Article
- Lateral Flow Assay for Hepatitis B Detection: A Review of Current and New Assays.Micromachines · 2023Review
- Evaluating anti-coronavirus activity of some phosphoramides and their influencing inhibitory factors using molecular docking, DFT, QSAR, and NCI-RDG studies.Journal of molecular structure · 2022Article
- The first coordination complex of (5Acta crystallographica. Section E, Crystallographic communications · 2021Article
- Synthesis of antimicrobial azoloazines and molecular docking for inhibiting COVID-19.Journal of heterocyclic chemistry · 2021Article
- The Dimroth Rearrangement in the Synthesis of Condensed Pyrimidines - Structural Analogs of Antiviral Compounds.Chemistry of heterocyclic compounds · 2021Article
- A novel protocol for catalyst-free synthesis of fused six-member rings to triazole and pyrazole.Molecular diversity · 2020Article
- Ultrasonic-assisted unusual four-component synthesis of 7-azolylamino-4,5,6,7-tetrahydroazolo[1,5-Beilstein journal of organic chemistry · 2020Article
- Development of Direct-acting Antiviral and Host-targeting Agents for Treatment of Hepatitis B Virus Infection.Gastroenterology · 2019Review
- In Vitro Anti-hepatitis B Virus Activity of 2',3'-Dideoxyguanosine.Virologica Sinica · 2018Article
- Review
- Effective DABCO-catalyzed synthesis of new tetrazolo[1,5-a]pyrimidine analogs.Molecular diversity · 2017Article
- Discovery and Mechanistic Study of Benzamide Derivatives That Modulate Hepatitis B Virus Capsid Assembly.Journal of virology · 2017Article
- Applicability of Metal Nanoparticles in the Detection and Monitoring of Hepatitis B Virus Infection.Viruses · 2017Review
- Development of Lateral Flow Assay Based on Size-Controlled Gold Nanoparticles for Detection of Hepatitis B Surface Antigen.Sensors (Basel, Switzerland) · 2016Article
- Treatment of hepatitis B virus: an update.Future microbiology · 2016Review
- Prediction of HBF-0259 interactions with hepatitis B Virus receptors and surface antigen secretory factors.Virusdisease · 2016Article
Corrections and comments
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Authors and funding
12 authors at 7 institutions in 2 countries.
Funding
Abstract
The high levels of hepatitis B virus (HBV) surface antigen (HBsAg)-bearing subviral particles in the serum of chronically infected individuals play an important role in suppressing HBV-specific immune response and are only mildly affected by the current small molecule therapies. Thus, a therapy that specifically reduces HBsAg serum levels could be used in combination therapy with nucleos(t)ide drugs or permit therapeutic vaccination for the treatment of HBV infection. Herein, we report the design, synthesis, and evaluation of novel triazolo-pyrimidine inhibitors (1, 3, and 4) of HBsAg cellular secretion, with activity against drug-resistant HBV variants. Extensive SAR led to substantial improvements in the EC(50) of the parent compound, 5 (HBF-0259), with the best being 3c, with EC(50) = 1.4 ± 0.4 μM, SI ≥ 36. The lead candidates, both 1a (PBHBV-001) and 3c (PBHBV-2-15), were well-tolerated in both normal and HBV-transgenic mice and exhibited acceptable pharmacokinetics and bioavailability in Sprague-Dawley rats.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.