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

• Published in: MedChemComm Vol. 12; no. 7; pp. 165 - 112
• Main Authors: Kaushik, Deepender, Kaur, Arshpreet, Petrovsky, Nikolai, Salunke, Deepak B
• Format: Journal Article
• Language: English
• Published: England Royal Society of Chemistry 21.07.2021; RSC
• Subjects: Agonists; Chemistry; Evolution; Imidazole; Imiquimod; TLR7 protein; Toll roads; Toll-like receptors; Vaccines

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 s...