Synthesis and Anti-inflammatory Evaluation of Novel Benzimidazole and Imidazopyridine Derivatives

Abstract

Sepsis, an acute inflammatory disease, remains the most common cause of death in intensive care units. A series of benzimidazole and imidazopyridine derivatives were synthesized and screened for anti-inflammatory activities, and the imidazopyridine series showed excellent inhibition of the expression of inflammatory cytokines in LPS-stimulated macrophages. Compounds <b>X10</b>, <b>X12</b>, <b>X13</b>, <b>X14</b>, and <b>X15</b> inhibited TNF-α and IL-6 release in a dose-dependent manner, and <b>X12</b> showed no cytotoxicity in hepatic cells. Furthermore, <b>X12</b> exhibited a significant protection against LPS-induced septic death in mouse models. Together, these data present a series of new imidazopyridines with potential therapeutic effects in acute inflammatory diseases