An article Selective Toll-like receptor 7 agonists with novel chromeno[3,4-d] imidazol-4(1H)-one and 2-(trifluoromethyl)quinoline/quinazoline-4-amine scaffolds WOS:000486133100009 published article about BIOLOGICAL EVALUATION; RECOGNITION; DERIVATIVES; ANTAGONISTS; ACTIVATION; DISCOVERY in [Dolsak, Ana; Svajger, Urban; Gobec, Stanislav; Sova, Matej] Univ Ljubljana, Fac Pharm, Askerceva 7, SI-1000 Ljubljana, Slovenia; [Svajger, Urban] Blood Transfus Ctr Slovenia, Slajmerjeva 6, SI-1000 Ljubljana, Slovenia; [Lesnik, Samo; Konc, Janez] Natl Inst Chem, Hajdrihova 19, SI-1000 Ljubljana, Slovenia in 2019, Cited 40. HPLC of Formula: C7H8N2O. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6
Toll-like receptors (TLRs) are promising targets for treatment of viral infections, autoimmune diseases, and cancers. Here, two new series of selective small-molecule TLR7 agonists with novel scaffolds and good selectivity over TLR8 are described, some with potencies in the low micromolar range. 8-Hydroxy-1-isobutylchromeno[3,4-d]imidazol-4(1H)-one (26) from the first series was designed and synthesized on the basis of previously described TLR7 antagonist 2, and is shown to be a selective TLR7 agonist (EC50, 1.8 mu M). The second series was based on 2-(trifluoromethyl)quinolin-4-amine and 2-(trifluoromethyl) quinazolin-4-amine scaffolds, which were defined according to our in-house ligand-based virtual screening protocol. Further synthesis of a focused library of analogs, biological evaluation, and docking studies provided systematic exploration of the structure-activity relationships, which indicate that a secondary or tertiary amine with smaller flexible alkyl substituents up to three carbon atoms in length, or bulkier rigid aliphatic rings is required at position 4 on 2-(trifluoromethyl)quinoline/quinazoline scaffold for potent TLR7 agonist activity. The influence of selected TLR7 agonists on cytokine production is also reported showing that N-cyclopropyl-2-(trifluoromethyl)quinazolin-4-amine (46) is able to induce increased levels of IL-6 and IL-8. These data demonstrate successful in-silico definition of novel TLR7 versus TLR8-selective compounds as promising chemical probes for further development of potent small-molecule immunomodulators. (C) 2019 Elsevier Masson SAS. All rights reserved.
HPLC of Formula: C7H8N2O. About 2-Aminobenzamide, If you have any questions, you can contact Dolsak, A; Svajger, U; Lesnik, S; Konc, J; Gobec, S; Sova, M or concate me.
Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem