24636-99-5

Upstream product

• 6269-89-2 1-(4-Nitrophenyl)piperazine 
• 105-36-2 ethyl bromoacetate 
• 105-39-5 chloroacetic acid ethyl ester 

Downstream Products

• 24636-90-6 2-[4-(4-nitrophenyl)piperazine-1-yl]acetohydrazide 

Relevant academic research and scientific papers

Novel azole-functionalited flouroquinolone hybrids: Design, conventional and microwave irradiated synthesis, evaluation as antibacterial and antioxidant agents

Background: The synthesis of new hybrid molecules consisting of several heterocyclic pharmacophores namely fluoroquinolone, 1,2,4-triazole, 1,3,4-oxadiazole and piperazine was carried out by conventional and successfully optimized microwave mediated techn

Newly synthesized piperazine derivatives as tyrosinase inhibitors: in vitro and in silico studies

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.

Synthesis of hydrazine containing piperazine or benzimidazole derivatives and their potential as α-amylase inhibitors by molecular docking, inhibition kinetics and in vitro cytotoxicity activity studies

The α-amylase is the main product of pancreas and is necessarily involved in the hydrolysis of carbohydrates into glucose so that it has been known to be a pioneer target for type 2 Diabetes mellitus (DM). Type 2 DM has no certain cure and the global increase in the cases of DM requires effective and extensive number of drug candidates. Drug discovery studies using organic biochemistry approaches are of important to describe novel compounds. This study aimed to reveal inhibitory potential of 13 novel compounds containing piperazine or benzimidazole moieties on α-amylase. The novel compounds were synthesized, structurally corroborated by various spectral analysis (FTIR, UV-Vis, 1H NMR and 13C NMR) and screened for anti α-amylase activity. Among the synthesized derivatives, compound 14 was found to be the most potent inhibitor of α-amylase having IC50 64.8 ± 1.8 μM. Inhibition types and Ki values of the most effective molecules (14 and 10a with different moieties) were further investigated. Molecular docking studies were conducted to correlate the outcome of in vitro biochemical kinetic assays and therefore rationalize the binding interactions. In vitro cytotoxicity studies on pancreatic cancer (AR42J) cells were then performed for compound14, and the compound was found to be more effective compared to the positive control, acarbose. Prediction of in silico ADME properties of all tested molecules were determined.

Design and synthesis of piperazine acetate podophyllotoxin ester derivatives targeting tubulin depolymerization as new anticancer agents

In this paper, a series of podophyllotoxin piperazine acetate ester derivatives were synthesized and investigated due to their antiproliferation activity on different human cancer cell lines. Among the congeners, C5 manifested prominent cytotoxicity towar

Design and synthesis of some piperazine hybrid molecules

In this work, a new series of piperazine hybrid molecules containing coumarin, isatin, salicyl, furane and 1,2,4-triazol-3- thiol moieties was synthesized in good yields. 2-[4-(4-Nitrophenyl)piperazin-1- yl]acetohydrazide was used as key intermediate to obtain these hybrid molecules. The structures of newly synthesized compounds were identified by 1H NMR, 13C NMR and elemental analysis data.

New N'-arylidene-2-[(4-nitrophenyl)piperazin-1-yl]acetohydrazide derivatives: Synthesis and anticancer activity investigation

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 %.

Synthesis and Biological Evaluation of Novel Piperazine Containing Hydrazone Derivatives

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.