BIOLOGICAL EVALUATION OF 1-(4-(HYDROXY(1-OXO-1,3-DIHYDRO-2H-INDEN-2-YLI-DENE)METHYL)PHENYL)-3-PHENYLUREA DERIVATIVES: ANTICHOLINERGICS AND ANTIEPILEPTIC POTENTIALS


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Koçyiğit Ü. M.

Fresenius Environmental Bulletin, cilt.4, ss.2739-2746, 2019 (SCI İndekslerine Giren Dergi)

  • Cilt numarası: 4 Konu: 28
  • Basım Tarihi: 2019
  • Dergi Adı: Fresenius Environmental Bulletin
  • Sayfa Sayıları: ss.2739-2746

Özet

In this work, a class of phenylurea compounds

containing 2-benzoylindan-1-one molecules 3a–3j

was designed and synthesized from the reaction of

phenylurea-substituted acetophenone compounds

with phthalaldehyde molecule under mild action situations

in good yields. The inhibitory effect of these

compounds on some metabolic enzymes was examined

and compared with a standard compound. IC50

values were obtained from the phenylurea-Induced

Activity (%)-[phenylurea compounds] graph and

from the Lineweaver-Burk graph. According to the

results, the IC50 values of these molecules were in

the range 18.23-63.01 nM for hCA I, while the mean

Ki values were in the range 7.79±0.94-122.64±32.15

nM for this enzyme. The results obtained are expected

to make an important contribution to drug design

and pharmacological applications. Additionally,

these compounds demonstrated well inhibitory

effects against acetylcholineesterase (AChE) enzyme.

Finally, the Ki values of hCA II were in the

range 15.09±4.48-65.72±6.64 nM and 1.54±0.21-

22.44±3.83 nM against AChE, respectively.