Synthesis of novel benzothiophene derivatives as protectors against cranial irradiation-induced neuroinflammation.

<b>Aim:</b> Cranial irradiation results in many deleterious effects to normal tissues, including neuroinflammation. There is a need to explore radioprotective agents that could be safely used to ameliorate these effects. <b>Method:</b> Nine novel benzothiophene derivatives bearing pyrimidinone, pyrazolidinone, triazole and other active moieties were synthesized and evaluated as antioxidants in an <i>in vitro</i> screening experiment. The most potent compounds were then tested as protectors against radiation-induced neuroinflammation and oxidative stress in rat brains following cranial irradiation. <b>Results:</b> The most potent antioxidant compounds were compounds 3-5 and 10 . P-fluro,p- bromo and pyrido benzothiophene derivatives offered good antioxidant and anti-inflammatory effects. <b>Conclusion:</b> Compounds 3-5 may be introduced as nontoxic candidates for adjuvant therapeutic protocols used in head and neck tumor radiotherapeutic management.