Bisarylthiourea comprising cycloalkyl-thiophene-3-carboxylate derivatives as potential Human Toll-Like Receptor (TLR)2 Agonists: Design, Synthesis, and Structure-Activity Relationship Enabling the Switch from TLR2/1 to TLR2/6 Activation

Key Points

• The study aims to develop bisarylthiourea derivatives as TLR2 agonists to enhance immune responses.
• Designed and synthesized cycloalkyl-thiophene-3-carboxylate derivatives.
• Evaluated structure-activity relationships for TLR2 activation.
• Tested both TLR2/1 and TLR2/6 activation pathways.
• Identified specific derivatives that preferentially activate TLR2/6 over TLR2/1.
• Demonstrated increased immunomodulatory effects with selected compounds.