Imidazopyrazines as New Anti‐inflammatory Agents: Discovery and Biological Activity Research in vitro and in vivo

Abstract

A series of imidazopyrazine derivatives were synthesized, and evaluated for their anti‐inflammatory activity in vitro and in vivo using RAW264.7 cells model and Zebrafish Traumatic Infection Inflammation model. The results in vitro showed that the compounds had significant inhibitory effect on inflammatory factor interleukin 6 (IL6), and N‐ (3 ‐( 4‐ ((1,1‐dioxidothiomorpholino) methyl)phenyl) imidazo [1,5‐a] pyrazin‐6‐yl) cyclopropanecarboxamide A1 the best activity, which was significantly different from that of the lipopolysaccharide (LPS) control group (P<0.03). The experiment of anti‐inflammatory activity in vivo indicated that compound A1 showed obvious aggregation inhibitory activity on inflammatory effector cells which was significantly different from that in the tail‐cutting control group (P<0.03). When the concentration of the compound was 160 μg/mL, the inhibitory activity of compound A1 was better than that of dexamethasone positive control group (P<0.05). This study could supply some anti‐inflammatory leading structure and possible mechanism for studying and developing new anti‐inflammatory agents.

Anti‐Herpes Simplex Virus Type 1 Activity Evaluation of Natural Derived Phloroglucinol Derivatives and Their Molecular Mechanisms Study

“…The compounds were provided by Guangdong Pharmaceutical University, which were prepared according to the references. [22][23][24][25][26][27]…”

“…The solvents and reagents were purchased from commercial vendors. The compounds were provided by Guangdong Pharmaceutical University, which were prepared according to the references [22–27] …”