Novel piperazine substituted indole derivatives: Synthesis, anti-inflammatory and antioxidant activities and molecular docking
Journal of Research in Pharmacy, cilt.24, sa.3, ss.350-360, 2020 (ESCI, Scopus, TRDizin)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 24 Sayı: 3
- Basım Tarihi: 2020
- Doi Numarası: 10.35333/jrp.2020.157
- Dergi Adı: Journal of Research in Pharmacy
- Derginin Tarandığı İndeksler: Emerging Sources Citation Index (ESCI), Scopus, TR DİZİN (ULAKBİM)
- Sayfa Sayıları: ss.350-360
- Anahtar Kelimeler: Anti-inflammatory activity, antioxidant activity, COX-2, piperazine, indole
- Sağlık Bilimleri Üniversitesi Adresli: Evet
Özet
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.