Design, Synthesis and Biological Screening of Novel 1,5-Diphenyl-3-(4-(trifluoromethyl)phenyl)-2-pyrazoline Derivatives


Tok F. , Kaymakçioğlu B.

Acta Chimica Slovenica, cilt.67, sa.4, ss.1139-1147, 2020 (SCI Expanded İndekslerine Giren Dergi)

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 67 Konu: 4
  • Basım Tarihi: 2020
  • Doi Numarası: 10.17344/acsi.2020.6028
  • Dergi Adı: Acta Chimica Slovenica
  • Sayfa Sayıları: ss.1139-1147

Özet

1-Phenyl-5-substituted-3-(4-(trifluoromethyl)phenyl)-4,5-dihydro-1H-pyrazole derivatives were synthesized from chalcone

derivatives. The structures of compounds were characterized by IR, 1H NMR spectroscopic methods and elemental

analysis. All compounds were evaluated for their in vitro antioxidant activity using DPPH and ABTS methods, anti-inflammatory

activity using lipoxygenase inhibitory method and antidiabetic activity using the α-glucosidase inhibitory

method. Especially, pyrazoline derivatives exhibited stronger anti-inflammatory activity than the reference drug indomethacin

(IC50: 50.45 μM) and their IC50 values were in the range of 0.68 and 4.45 μM. In addition, the ADME properties

of all chalcone and pyrazoline derivatives were calculated by Lipinski’s and Veber’s rules.