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