Structural evolution of toll-like receptor 7/8 agonists from imidazoquinolines to imidazoles

D Kaushik, A Kaur, N Petrovsky… - RSC Medicinal Chemistry, 2021 - pubs.rsc.org
Several synthetic heterocyclic small molecules like imiquimod, resiquimod, CL097, CL075,
bromopirone, tilorone, loxoribine and isatoribine demonstrated TLR7/8 agonistic activity and …

Discovery of benzimidazole substituted 1, 2, 4-oxadiazole compounds as novel anti-HBV agents with TLR8-agonistic activities

J Qiu, Y Zou, S Li, L Yang, Z Qiu, F Kong… - European Journal of …, 2022 - Elsevier
Hepatitis B virus (HBV) infection is a public health threat worldwide and characterized by a
dysfunctional immune response. In the present work, a new series of benzimidazole …

2, 4-Diaminoquinazolines as dual toll-like receptor (TLR) 7/8 modulators for the treatment of hepatitis B virus

W Embrechts, F Herschke, F Pauwels… - Journal of Medicinal …, 2018 - ACS Publications
A novel series of 2, 4-diaminoquinazolines was identified as potent dual Toll-like receptor
(TLR) 7 and 8 agonists with reduced off-target activity. The stereochemistry of the amino …

Suzuki–Miyaura cross‐coupling

AB Pagett, GC Lloyd‐Jones - Organic Reactions, 2004 - Wiley Online Library
The Suzuki–Miyaura cross coupling reaction uses a metal catalyst to create carbon–carbon
bonds from organoboron reagents and organo (pseudo) halides. By careful adjustment of …

TLR7 modulating B-cell immune responses in the spleen of C57BL/6 mice infected with Schistosoma japonicum

H Wei, H Xie, J Qu, A Xie, S Xie, H Huang… - PLoS Neglected …, 2021 - journals.plos.org
B cells played an important role in Schistosoma infection-induced diseases. TLR7 is an
intracellular member of the innate immune receptor. The role of TLR7 on B cells mediated …

The efficacy of a 2,4-diaminoquinazoline compound as an intranasal vaccine adjuvant to protect against influenza A virus infection in vivo

K Noh, EJ Jeong, T An, JS Shin, H Kim, SB Han… - Journal of …, 2022 - Springer
Adjuvants are substances added to vaccines to enhance antigen-specific immune
responses or to protect antigens from rapid elimination. As pattern recognition receptors, Toll …

Design and synthesis of novel quinazolinone derivatives as anti-HBV agents with TLR8 agonist effect

J Qiu, Q Zhou, Y Zou, S Li, L Yang, W Chen… - European Journal of …, 2022 - Elsevier
Hepatitis B virus (HBV) infection is a worldwide threat to public health. In this work, a series
of novel quinazolinone derivatives (5a-q) were synthesized and evaluated as novel anti …

TLR7 Modulated T Cell Response in the Mesenteric Lymph Node of Schistosoma japonicum‐Infected C57BL/6 Mice

J Qu, X Yu, C Jin, Y Feng, S Xie, H Xie… - Journal of …, 2019 - Wiley Online Library
Toll‐like receptors (TLRs) play an important role in regulating immune responses during
pathogen infection. However, roles of TLRs on T cells reside in the mesenteric lymph node …

Subtle differences in chemical pattern between human toll‐like receptor 8 agonists and antagonists: Emerging chemical patterns analysis

S Huang, H Mei, D Zhang, T Shi, L Chen… - Chemical Biology & …, 2019 - Wiley Online Library
Due to the potencies in the treatments of cancer, infectious diseases, and autoimmune
diseases, the developments of human TLR8 (hTLR8) agonists and antagonists have …

The emerging chemical patterns applied in predicting human toll-like receptor 8 agonists

S Huang, H Mei, D Zhang, Y Ren, MY Kevin, X Pan - MedChemComm, 2018 - pubs.rsc.org
Toll-like receptors (TLRs) are important pattern recognition receptors to human innate
immunity, which can recognize pathogen-associated molecular patterns and initiate innate …