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

摘要

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. IC_(50) values were obtained from the phenylurea-Induced Activity ()-phenylurea compounds graph and from the Lineweaver-Burk graph. According to the results, the IC_(50) 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 Ki values of hCA II were in the range15.09±4.48-65.72±6.64nMand1.54±0.21- 22.44±3.83 nM against AChE, respectively.