Synthesis and antioxidant activity of some 1-aryl/aralkyl piperazine derivatives with xanthine moiety at N4

Abstract

Piperazine nucleus is one of the most important heterocyclic systems exhibiting remarkable pharmacological activities. Thus, in the current study six new aryl/aralkyl substituted piperazine derivatives, containing methylxanthine moiety were synthesized and their structures were confirmed by IR and 1H NMR analysis. All compounds were in vitro screened for their activity as antioxidants using DPPH (2,2′-Diphenyl-1-picrylhydrazyl), ABTS (2,2′-azinobis-(3-ethylbenzo thiazine-6-sulfonic acid)) and FRAP (ferric reducing/antioxidant power) methods. The antioxidant activity of the studied compounds against lipid peroxidation was also measured. The highest antioxidant activity was demonstrated by compound 3c. It is obvious that the presence of a hydroxyl group in the structure is essential for the antioxidant properties and should be taken into consideration in further design of structures with potential antioxidant properties.

Molecular Docking Study on 1-(3-(4-Benzylpiperazin-1-Yl)propyl)-3,7-Dimethyl-1h-Purine-2,6(3h,7h)-Dione as an Acetylcholinesterase Inhibitor

“…The evaluated structure was obtained according to a synthetic procedure (Andonova et al, 2014) presented in Figure 4. In an attempt to obtain preliminary information on some physicochemical properties of the targeted structure, the LA1 molecule was theoretically evaluated by some of the parameters of Lipinski's Rule of Five including molecular weight, miLogP, number of hydrogen bong donators (nOHNH) and hydrogen bond acceptors (nON) calculated by Molinspiration cheminformatics.…”

“…The evaluated structure was obtained according to a synthetic procedure described in Andonova et al, 2014.…”

In vitro mutagenic, antimutagenic, and antioxidant activities evaluation and biotransformation of some bioactive 4‐substituted 1‐(2‐methoxyphenyl)piperazine derivatives

“…All the tests were run in triplicates and the values were averaged. Compounds ability to scavenge DPPH radical was calculated by the following equation: Scavenging effect (%) = (( Ac – As )/ Ac ) × 100, where Ac is the absorbance of the control reaction (DPPH solution with methanol) and As is the absorbance of the test compound in the presence of DPPH solution …”

Virtual Toxicity and Drug Likeness of Newly Synthesized Methylxanthines With N1 Arylpiperazine Moiety

“…In the presented research we evaluate the potential risk of a group of 12 methylxanthines, containing an arylpiperazine moiety at N 1 (Scheme 1, series 1, compounds 1a-e and series 2, compounds 2a-e) using the online hazard-screening tool-PBT Profiler (http://www.pbtprofiler.net/). Scheme 1: Structures of methylxanthines, containing an arylpiperazine moiety at N 1 , obtained by the previously described procedure (Andonova, 2014) Source: Author PBT Profiler is a screening server that uses the limits published in the EPA (United States Environmental Protection Agency) to automatically identify compounds that are potentially persistent in the environment and capable of bioaccumulation in the food chain. The results for assessing the stability, bioaccumulation and toxicity of compounds 1a-f and 2a-f are presented in Table 1.…”