ReviewRSC medicinal chemistry2021
Structural evolution of toll-like receptor 7/8 agonists from imidazoquinolines to imidazoles.
Review in RSC medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
20 citing papers in PubMed, 38 citations in OpenAlex.
- Ganoderma lucidum spore powder enhances IFN-α-mediated antiviral capacity of COVID-19 vaccine boosters revealed by single-cell multi-omics sequencing.Journal of advanced research · 2026Article
- Physicochemical and Biological Characterization of the TLR7 Agonist SZU-106.Pharmaceutical research · 2026Article
- Encapsulation of the lipidated TLR7/8 agonist INI-4001 into ionic liposomes impacts H7 influenza antigen-specific immune responses.Drug delivery and translational research · 2026Article
- Review
- 5'-tRNABiophysical journal · 2025Article
- Unlocking the power of imidazoquinolines: recent advances in anticancer and immunotherapeutic strategies.Future medicinal chemistry · 2025Review
- Efflux-Enhanced Imidazoquinolines To Exploit Chemoresistance.ACS omega · 2025Article
- The recent advances in vaccine adjuvants.Frontiers in immunology · 2025Review
- Toll-like receptor agonists as cancer vaccine adjuvants.Human vaccines & immunotherapeutics · 2024Review
- Linker Chemistry and Connectivity Fine-Tune the Immune Response and Kinetic Solubility of Conjugated NOD2/TLR7 Agonists.Bioconjugate chemistry · 2024Article
- Interleukin-1 receptor-associated kinase 4 (IRAK4) is a critical regulator of inflammatory signalling through toll-like receptors 4 and 7/8 in murine and human lungs.British journal of pharmacology · 2024Article
- Modulation of the Adjuvant Potential of Imidazoquinoline-Based TLR7/8 Agonists via Alum Adsorption.ACS medicinal chemistry letters · 2024Article
- Design and Synthesis of Polyphenolic Imidazo[4,5-ACS pharmacology & translational science · 2024Article
- Structure-activity relationship in NOD2 agonistic muramyl dipeptides.European journal of medicinal chemistry · 2024Review
- Identification and Optimization of Small Molecule Pyrazolopyrimidine TLR7 Agonists for Applications in Immuno-oncology.ACS medicinal chemistry letters · 2024Article
- Unveiling the multifaceted role of toll-like receptors in immunity of aquatic animals: pioneering strategies for disease management.Frontiers in immunology · 2024Review
- Small molecule modulators of immune pattern recognition receptors.RSC chemical biology · 2023Review
- Synthesis and immunopharmacological evaluation of novel TLR7 agonistic triazole tethered imidazoquinolines.RSC advances · 2023Article
- Toll-like receptors and toll-like receptor-targeted immunotherapy against glioma.Journal of hematology & oncology · 2021Review
- Role of toll-like receptor 7/8 pathways in regulation of interferon response and inflammatory mediators during SARS-CoV2 infection and potential therapeutic options.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2021Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Several synthetic heterocyclic small molecules like imiquimod, resiquimod, CL097, CL075, bromopirone, tilorone, loxoribine and isatoribine demonstrated TLR7/8 agonistic activity and relatively modest structural changes in such molecules result in major variation in the TLR7 and/or TLR8 activity. A strict dependency of the electronic configuration of the heterocyclic system was also observed to influence the agonistic activity. In the present review, an evolution of imidazole based TLR7/8 agonist from imidazoquinoline based scaffold is delineated along with the elaboration of detailed structure activity relationship (SAR) in each chemotype. The structural and activity details of not only the active compounds but also the related inactive compounds are included to better understand the SAR. TLR7/8 agonists are emerging as promising vaccine adjuvant candidates and the present SAR and structural information will provide a road map towards the identification of more potent and appropriate candidates for further drug discovery.
Identifiers
What Socratic holds
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 Socratic graph.