24636-90-6Relevant articles and documents
Synthesis and Biological Evaluation of Novel Piperazine Containing Hydrazone Derivatives
Kaya, Betül,?zkay, Yusuf,Temel, Halide Edip,Kaplancikli, Zafer Asim
, (2016)
Some hydrazone derivatives were synthesized and their potential anticholinesterase activities were examined. A series of eleven new compounds of N′-(2,4-disubstitutedbenzylidene)-2-(4-(4-nitrophenyl)piperazin-1-yl)acetohydrazide derivatives were obtained via reaction of 2-[4-(4-nitrophenyl)piperazin-1-yl]acetohydrazide with aromatic aldehydes. The chemical structures of the compounds were enlightened by FT-IR, 1H-NMR, 13C-NMR, and HRMS (ESI) spectral data. The inhibition potency of the compounds 3a-k against AChE and BuChE was measured and evaluated using a modification of Ellman's spectrophotometric method. Among the tested compounds, compound 3c was assigned to be the most active derivative. Galantamine was used as a standard drug.
Newly synthesized piperazine derivatives as tyrosinase inhibitors: in vitro and in silico studies
Basoglu Ozdemir, Serap,Colak, Ahmet,Demir, Ilke,Dokuzparmak, Cigdem,Kurnaz, Busra,Oz Tuncay, Fulya,Sag Erdem, Safiye,Yildirim, Nuri
, (2022/01/24)
In this study, a series of new organic compounds with piperazine as a fundamental skeleton was synthesized and evaluated for their tyrosinase inhibitory potentials by in vitro and in silico studies. The in vitro studies have shown that compounds 10a and 10b bearing 1,2,4, triazole nucleus could be considered potent tyrosinase inhibitors with IC50 values of 31.2 ± 0.7 and 30.7 ± 0.2?μM, respectively. 10b (Ki = 9.54?μM, mixed type inhibition) with the lowest IC50 value among derivatives was selected to determine kinetic constants and inhibition types. Furthermore, molecular docking analysis was performed for all compounds and it was observed that 4b, 5a, 4c, and 10b showed promising inhibitory effect on tyrosinase activity. Based on docking results, ADME predictions and in vitro studies, 10b might be considered suitable oral drug candidates for further studies.
New N'-arylidene-2-[(4-nitrophenyl)piperazin-1-yl]acetohydrazide derivatives: Synthesis and anticancer activity investigation
Yurttas, Leyla,Kaplancikli, Zafer A.,Sennur, Gorgulu-Kahyaoglu
, p. 910 - 917 (2017/08/29)
Background: Compounds bearing ortho-hydroxy N-acyl hydrazone moiety have been reported with high anticancer activity acting by increasing the enzymatic activity of procaspase-3 in cancer cells and therefore inducing apoptosis in some tumour models. Methods: Considering this subunit's proclivity for anticancer activity we have synthesized novel N'-arylidene-2-[(4-nitrophenyl)piperazin-1-yl]acetohydrazide derivatives (3a-3n) including N-acyl hydrazone moiety with a well-known three step synthetic procedure. The antiproliferative activity of the compounds were investigated using MTT method and xCELLigence real time cell analysis system against NIH/3T3 (Mouse embryo fibroblast cell line) as healthy cell line and A549 (Human lung adenocarcinoma ephitelial cell line) as tumour cell line. Results and Conclusion: The IC50 values of final compounds were determined for 24h and 48h incubation periods. As a second stage, flow cytometric analysis was performed for selected highly active compounds (3g, 3i, 3j, 3n) on A549 cell line. Compound 3i bearing 3-chlorophenyl moiety was detected to cause apoptosis in a ratio of 54.7 %.
