So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Mackman, Richard L.; Mish, Michael; Chin, Gregory; Perry, Jason K.; Appleby, Todd; Aktoudianakis, Vangelis; Metobo, Sammy; Pyun, Peter; Niu, Congrong; Daffis, Stephane; Yu, Helen; Zheng, Jim; Villasenor, Armando G.; Zablocki, Jeff; Chamberlain, Jason; Jin, Haolun; Lee, Gary; Suekawa-Pirrone, Kimberley; Santos, Rex; Delaney, William E.; Fletcher, Simon P. researched the compound: 2-Aminoquinazolin-4(3H)-one( cas:20198-19-0 ).Name: 2-Aminoquinazolin-4(3H)-one.They published the article 《Discovery of GS-9688 (Selgantolimod) as a Potent and Selective Oral Toll-Like Receptor 8 Agonist for the Treatment of Chronic Hepatitis B》 about this compound( cas:20198-19-0 ) in Journal of Medicinal Chemistry. Keywords: CHB TLR8 agonist optimization binding HBV DNA RNA. We’ll tell you more about this compound (cas:20198-19-0).
Toll-like receptor 8 (TLR8) recognizes pathogen-derived single-stranded RNA fragments to trigger innate and adaptive immune responses. Chronic hepatitis B (CHB) is associated with a dysfunctional immune response, and therefore a selective TLR8 agonist may be an effective treatment option. Structure-based optimization of a dual TLR7/8 agonist led to the identification of the selective TLR8 clin. candidate (R)-2-((2-amino-7-fluoropyrido[3,2-d]pyrimidin-4-yl)amino)-2-methylhexan-1-ol (GS-9688, (R)-7)(I). Potent TLR8 agonism (IL-12p40 EC50 = 220 nM) and >100-fold TLR7 selectivity (IFN-α EC50 > 50μM) was observed in human peripheral blood mononuclear cells (PBMCs). The TLR8-ectodomain:(R)-7 complex confirmed TLR8 binding and a direct ligand interaction with TLR8 residue Asp545. Oral (R)-7 had good absorption and high first pass clearance in preclin. species. A reduction in viral markers was observed in HBV-infected primary human hepatocytes treated with media from PBMCs stimulated with (R)-7, supporting the clin. development of (R)-7 for the treatment of CHB.
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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis