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

KOÇYİĞİT Ü. M.

FRESENIUS ENVIRONMENTAL BULLETIN, cilt.28, sa.4, ss.2739-2746, 2019 (SCI-Expanded) identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 28 Sayı: 4
  • Basım Tarihi: 2019
  • Dergi Adı: FRESENIUS ENVIRONMENTAL BULLETIN
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED)
  • Sayfa Sayıları: ss.2739-2746
  • Anahtar Kelimeler: Phenylurea, carbonic anhydrase, acetylcholinesterase, enzyme inhibition, antiepileptic potentials, CARBONIC-ANHYDRASE, INHIBITORY PROPERTIES, CRYSTAL-STRUCTURE, ACETYLCHOLINESTERASE, ANTIOXIDANT, ESTERASE
  • Sivas Cumhuriyet Üniversitesi Adresli: Evet

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 K-i 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 K-i 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.