The present disclosure relates to a novel small molecule TLR2 antagonist, and particularly, to 19 novel TLR2 antagonists, a pharmaceutical composition, including the antagonists, for preventing or treating inflammatory diseases, and a TLR4 regulator.The novel TLR2 antagonists according to the present disclosure can be effectively used as a preparation for oral administration by having low molecular weight and high oral bioavailability, and can be useful in pharmaceutical compositions for preventing or treating inflammatory diseases since the secretion of IL-8 is effectively inhibited and in vivo cytotoxicity is not induced. In addition, the novel TLR2 antagonists according to the present disclosure can be used as a TLR4 regulator.
