Bioisosteric modification on melatonin: Synthesis of new naphthalene derivatives, in vitro antioxidant activity and cytotoxicity studies


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Shirinzadeh H., Ghalia M., Tascioglu A., Adjali F. I., Gunesacar G., Gurer-Orhan H., ...Daha Fazla

Brazilian Journal of Pharmaceutical Sciences, cilt.56, ss.1-11, 2020 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 56
  • Basım Tarihi: 2020
  • Doi Numarası: 10.1590/s2175-97902019000418124
  • Dergi Adı: Brazilian Journal of Pharmaceutical Sciences
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, BIOSIS, CAB Abstracts, EMBASE, Veterinary Science Database, Directory of Open Access Journals
  • Sayfa Sayıları: ss.1-11
  • Anahtar Kelimeler: Antioxidant, Cytotoxic, Melatonin, MTT, DPPH, OXIDATIVE STRESS, PHARMACOLOGICAL EVALUATION, ANALOGS, AGOMELATINE, SERIES, HYDRAZONES, REDUCTION, RELEASE, DESIGN, BRAIN
  • Erzincan Binali Yıldırım Üniversitesi Adresli: Evet

Özet

© 2020, Faculdade de Ciencias Farmaceuticas (Biblioteca). All rights reserved.Melatonin (MLT) is a strong free radical scavenger that protects the body from the deleterious effects of excess oxidants. Synthesis of MLT analogue compounds with antioxidant potency has recently attracted the interest of researchers. In general, the strategy consists of modifying the groups in the different sites of the indole ring or replacing the indole ring with an analogue. As part of our ongoing research, the antioxidant capacity and cytotoxicity of newly synthesized MLT analogue naphthalene derivatives were evaluated. The radical scavenging activity was tested by a 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay. Most of the synthesized compounds showed significant antioxidant activity in comparison to MLT. The structure-activity relationship was identified. The in vitro cytotoxic effects of the synthesized compounds were also investigated in CHO-K1 cells using the MTT assay.