Novel piperazine substituted indole derivatives: Synthesis, anti-inflammatory and antioxidant activities and molecular docking

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Altuntas T., Baydar A., KILIÇ KURT Z., Acar C., YILMAZ SARIALTIN S., ÇOBAN T.

JOURNAL OF RESEARCH IN PHARMACY, cilt.24, sa.3, ss.350-360, 2020 (ESCI) identifier identifier identifier

  • 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, OXIDATIVE STRESS, SCAVENGING ACTIVITY, INFLAMMATION, DRUG, INDOMETHACIN, DISCOVERY, RELEASE
  • Ankara 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.