Editor-in-Chief Hatice Kübra Elçioğlu Vice Editors Levent Kabasakal Esra Tatar Online ISSN 2630-6344 Publisher Marmara University Frequency Bimonthly (Six issues / year) Abbreviation J.Res.Pharm. Former Name Marmara Pharmaceutical Journal
Journal of Research in Pharmacy 2020 , Vol 24 , Issue 3
Novel piperazine substituted indole derivatives: Synthesis, anti-inflammatory and antioxidant activities and molecular docking
Tunca Gül ALTUNTAŞ1,Aziz BAYDAR1,Zühal KILIÇ-KURT1,Cemre ACAR1,Sezen YILMAZ-SARIALTIN2,Tülay ÇOBAN2
1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, Ankara, Turkey
2Department of Pharmaceutical Toxicology, Faculty of Pharmacy, Ankara University, Ankara, Turkey
DOI : 10.35333/jrp.2020.157 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. Keywords : Anti-inflammatory activity; antioxidant activity; COX-2; piperazine; indole
Marmara University