24636-99-5Relevant articles and documents
Novel azole-functionalited flouroquinolone hybrids: Design, conventional and microwave irradiated synthesis, evaluation as antibacterial and antioxidant agents
Mentese, Meltem,Demirbas, Neslihan,Mermer, Arif,Demirci, Serpil,Demirbas, Ahmet,Ayaz, Faik Ahmet
, p. 46 - 64 (2018)
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
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
Cakmak, Ummuhan,Oz-Tuncay, Fulya,Basoglu-Ozdemir, Serap,Ayazoglu-Demir, Elif,Demir, ?lke,Colak, Ahmet,Celik-Uzuner, Selcen,Erdem, Safiye Sag,Yildirim, Nuri
, p. 1886 - 1904 (2021/08/23)
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 some piperazine hybrid molecules
Yilmaz, Fatih,Mente?e, Meltem
, p. 941 - 946 (2018/04/09)
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.
