NOVEL PIPERAZINE SUBSTITUTED INDOLE DERIVATIVES: SYNTHESIS, ANTI-INFLAMMATORY AND ANTIOXIDANT ACTIVITIES AND MOLECULAR DOCKING

TUNCA GÜL ALTUNTAŞ, AZİZ BAYDAR, ZÜHAL KILIÇ-KURT, CEMRE ACAR, SEZEN YILMAZ-SARIALTIN, TÜLAY ÇOBAN

Journal of Research in Pharmacy - 2020;24(3):350-360

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, Ankara, Turkey

 

In this work, a series of piperazine substituted indole derivatives were synthesized and evaluated for their in vitro antioxidant and anti-inflammatory activities. The results of antioxidant activity showed that compounds 2 (81.63%) and 11 (85.63%) had comparable DPPH free radical scavenging activity to Vit E (88.6%). The in vitro anti-inflammatory assays indicated that most of the compounds had more higher anti-inflammatory activities than standart ASA. Docking results revealed that compound 11 possessing the strongest anti-inflammatory activities showed the H-bond interactions with the key residues of COX-2 active site. It suggested that the anti-inflammatory activity of the compounds might result from COX-2 inhibition. It will be verified with further enzyme inhibition assays.