High Purities Research Articles

Hydrothermally Synthesized Hydroxyapatite-Silica Composites with Enhanced Mechanical Properties for Bone Graft Applications

The demand for synthetic bone grafts has increased in recent years. Hydroxyapatite (HA) is one of the highly suitable candidates as a bone graft material due to its excellent biocompatibility and high osteoconductive properties with low toxicity. HA has disadvantageous mechanical strength showing relatively fragile and brittle behavior due to its high hygroscopic properties. This leads to improper mechanical properties for such grafting applications. Therefore, HA should be combined with another material with similar biocompatibility and high hardness, such as SiO2. In this work, HA/SiO2 (HAS) composite material was prepared via a hydrothermal method to obtain the high purities of HA with a particle size of approximately 35 nm and around 50% crystallinity. It was found that the addition of SiO2 stimulated the composite system by forming an orthosilicic acid complex that can reduce the overall solution’s pH, thus contributing to the integrity and stability of the HAS composite. Therefore, higher SiO2 contents in the HAS composite can enhance its mechanical stability when immersed in simulated body fluid (SBF). Our work demonstrated that HAS can highly improve HA material’s hardness and mechanical stability under immersion of SBF. The Vickers test showed that the 0.05 GPa hardness in 10% SiO2 increased to 0.35 GPa hardness with the addition of 20% SiO2. The crystal structures of HAS were analyzed using X-ray diffraction, and the morphology of the HAS composites was observed under electron microscopy.

Synthesis and Preclinical Evaluation of Fluorinated 5-Azaindoles as CB2 PET Radioligands.

Several classes of cannabinoid receptor type 2 radioligands have been evaluated for imaging of neuroinflammation, with successful clinical translation yet to take place. Here we describe the synthesis of fluorinated 5-azaindoles and pharmacological characterization and in vivo evaluation of 18F-radiolabeled analogues. [18F]2 (hCB2 Ki = 96.5 nM) and [18F]9 (hCB2 Ki = 7.7 nM) were prepared using Cu-mediated 18F-fluorination with non-decay-corrected radiochemical yields of 15 ± 6% and 18 ± 2% over 85 and 80 min, respectively, with high radiochemical purities (>97%) and molar activities (140-416 GBq/μmol). In PET imaging studies in rats, both [18F]2 and [18F]9 demonstrated specific binding in CB2-rich spleen after pretreatment with CB2-specific GW405833. Moreover, [18F]9 exhibited higher brain uptake at later time points in a murine model of neuroinflammation compared with a healthy control group. The results suggest further evaluation of azaindole based CB2 radioligands is warranted in other neuroinflammation models.

Recovery of platinum group metals from aqueous solution by iron-electrocoagulation

The recovery of platinum group-metals (PGMs) has attracted increasing attention owing to their scarcity, economic importance, and criticality. Traditional techniques for PGM recovery often involve the use of toxic reagents and require strict extraction conditions, posing challenges for their implementation in complex environments. In this paper, a novel method based on iron electrocoagulation (Fe-EC) is proposed for PGM extraction. The Fe-EC process generates iron (hydr)oxide flocs in situ, which spontaneously and uniformly adsorb and reduce PGM ions. The selectivity of PGM recovery is attributed to the higher electronegativity and standard reduction potential of PGM ions compared to base metal ions. Efficient extraction of Pt, Pd, and Rh ions from aqueous solutions was achieved using Fe-EC, with extraction efficiencies of 81.26 %, 81.32 %, and 99.66 %, respectively. These results were obtained at a voltage of 2 V and residual concentrations of 0.3072, 0.0051 and 0.0049 mg L–1. TEM-EDS and XPS characterizations of the Fe-EC flocs showed that Pt, Pd, and Rh were present in the elemental form particles. The extraction performance of base metal such as Ni, Zn, Mg and Mn ions by Fe-EC was found to be poor, with minimal reduction to elemental form. Finally, the Fe-EC flocs were subjected to acid washing and filtration, resulting in the selective recovery of Pt, Pd, and Rh products with high purities of 97.43%, 97.12%, and 97.92%, respectively. This study presents a new and environmentally friendly method for the recycling of PGMs, offering a promising approach for sustainable PGM recovery.

Iridium-Catalyzed asymmetric reduction of α,β-Unsaturated nitriles with water

The nitrile compounds are present in a variety of biologically active natural products and pharmaceuticals, and the nitrile groups are versatile synthetic intermediates to other functionalized compounds. Herein, the asymmetric reduction of α,β-unsaturated nitriles with water as a hydrogen source is reported. The reaction is catalyzed by the complex of [Ir(COD)Cl]2 and (Ra, S)-Ph-Bn-SiPhox, and allows the preparation of useful enantioenriched chiral 3,3-disubstituted propionitriles with high optical purities in mild conditions.

Influence of elements (Zr, Mo, Cr, Fe, and Ni) doping on the electromagnetic wave absorption performance of Ti3AlC2-based ceramics

Currently, materials that absorb electromagnetic waves (EMW) are being increasingly studied and used. In particular, numerous attempts have been made to improve the performance of EMW-absorbing ceramics, but little attention was paid to the effect of doping on their relevant properties. In this work, Ti3AlC2, a typical MAX-phase ceramic, was doped with different elements (Zr, Mo, Cr, Fe and Ni) at the M site via a pressure-free reactive sintering. Phase and microstructure analysis show that the doped Ti3AlC2 samples possess high purities and typical layered structures. It was noticed that (Ti0.8Zr0.2)3AlC2 demonstrates the lowest reflection loss (−48.0 dB at the thickness of 1.62 mm) and a maximum effective absorption bandwidth of 3.9 GHz. Elemental doping has been proved to alter the dielectric and magnetic properties of Ti3AlC2, and the boosted EMW absorption performance was found to be originated from the improved impedance matching. Here, we systematically investigated the influence of different dopants on the EMW absorption characteristics of Ti3AlC2, which provides significant insights for the future design of novel EMW-absorbing materials.

Asymmetric tandem conjugate addition and reaction with carbocations on acylimidazole Michael acceptors.

We present here a stereoselective tandem reaction based on the asymmetric conjugate addition of dialkylzinc reagents to unsaturated acylimidazoles followed by trapping of the intermediate zinc enolate with carbocations. The use of a chiral NHC ligand provides chiral zinc enolates in high enantiomeric purities. These enolates are reacted with highly electrophilic onium compounds to afford densely substituted acylimidazoles. DFT calculations helped to understand the reactivity of the zinc enolates derived from acylimidazoles and allowed their comparison with metal enolates obtained by other conjugate addition reactions.

Preparation of TiO2 pigment from ilmenite ore concentrate by molten alkaline process

TiO2 pigment production from an ilmenite concentrate via a molten alkaline process was investigated. The ilmenite concentrate (54.19% TiO2) was first roasted in the molten NaOH system at various temperatures ranging from 600 to 800°C while the mass ratio of NaOH/ilmenite was varied within the range of 0.8-1.2 for 1 hour. The achieved roasted efficiency was up to 93.93% at a temperature of 700°C and NaOH/ilmenite ratio of 1:1. The roasted product was first leached in water and then in a solution of HCl 20% at 50ºC for 2 hours. The TiOCl2 solution was hydrolysed at 95oC for 2 hours. Precipitation of the hydrolysis process was then calcinated at 800oC. The final obtained product contained up to 96.37% of TiO2. Ilmenite can be used as a raw material in a molten alkaline process. It is obvious that not only high purities of TiO2 could be achieved, but also the reduction of waste materials, raw materials, energy, and time.

Sugarcane Straw as a Source of Arabinoxylans: Optimization and Economic Viability of a Two-Step Alkaline Extraction.

Sugarcane processing produces a significant amount of byproducts in the form of straw and bagasse, which are rich in cellulose, hemicellulose, and lignin. This work aims to provide a valorization approach to sugarcane straw by optimizing a two-step alkaline extraction of arabinoxylans by a response surface methodology to evaluate a potential industrial-scale production. Sugarcane straws were delignified using an alkaline-sulfite pretreatment, followed by alkaline extraction and precipitation of arabinoxylan, a two-step process optimized using a response surface methodology. A KOH concentration of (2.93-17.1%) and temperature (18.8-61.2 °C) were chosen as independent variables, and the arabinoxylan yield (%) as a response variable. The model application shows that KOH concentration, temperature, and the interaction between both independent variables are significant in extracting arabinoxylans from straw. The best-performing condition was further characterized by FTIR, DSC, and chemical and molecular weight evaluation. The straws arabinoxylans presented high purities levels, ca. 69.93%, and an average molecular weight of 231 kDa. The overall estimated production cost of arabinoxylan from straw was 0.239 €/g arabinoxylan. This work demonstrates a two-step alkaline extraction of the arabinoxylans method, as well as their chemical characterization and economic viability analysis, that can be used as a model for industrial scale-up production.

Preliminary biological evaluations of first brain‐penetrant GPR119‐based radiotracer in rodents and non‐human primates

AbstractBackgroundG‐protein‐coupled receptors (GPCRs) plays a key role in regulating glucose metabolism. While GPR119 (an important GPCR) agonists have shown potential for improving neurologic and cognitive function in patients with AD and type2 diabetes mellitus (T2DM), clinical interventions targeting GPR119 will require accurate in vivo measures such as PET imaging. We recently synthesized a series of novel piperdine analogs, identifying two analogs (T1 and T2) with high GPR119 binding potency (2‐5 nM) for PET radiochemistry. Here we report their radiochemistry and initial biological evaluations in neuronal cells, normal rodents, and monkeys (vervets).Method[18F]T1/T2 radiochemistry was performed in TRASIS‐AIO automated module following [18F]¯‐based nucleophilic substitution of corresponding precursors. [18F]T1 and T2 in vitro assays were performed in three patient‐derived cell lines with different GPR119 expression (MDM‐MD‐231<NCI‐H1716<HepG2), with and without GPR119 agonists and non‐radioactive T1/T2. Dynamic 0‐60 min brain microPET/CT imaging and biodistribution were performed in normal balb/c mice (n = 4). Healthy adult female vervets (n = 6, 4.5‐6.7 kg) underwent 0‐90 min brain PET imaging. Standard uptake value (SUVmax) and time‐activity curves (TACs) were calculated for whole brain PET/MR images.ResultBoth [18F]T1 and T2 were produced in high radiochemical purities (>98%) and specific activities (∼3800‐4500 mCi/µmol), decay corrected to end of synthesis. Radioactive cell uptake was lower in MDM‐MD‐231 cells (lowest GPR119 expression) and higher in HepG2 cells (higher GPR119 expression); uptake also significantly increased with GPR119 agonists and T1/T2 treatments compared to baseline. [18F]T2 showed slightly better brain uptake in mice compared to [18F]T1 (SUVmax = 0.35±0.07 Vs. 0.55±0.09 g/mL). Biodistribution of [18F]T2 (%ID/mg = 1.01±0.09) also showed high brain uptake. SUVmax (avg = 2.6±0.1 g/mL) and TACs of both [18F]T1 and [18F]T2 in monkey brains demonstrated rapid distribution across BBB within 10 min and favorable clearance within 90 min of tracer injection (Fig 1).ConclusionRadiochemistry was successfully automated and optimized. Cell uptake showed direct relationships between radiotracer uptake and GPR119 expression. MicroPET imaging, biodistribution in rodents and monkey PET imaging demonstrated excellent brain uptake and favorable pharmacokinetics, indicating BBB penetration. These data suggest for the first time that [18F]T1 and T2 have potential for imaging GPR119 in brains of humans with AD or T2DM.

Cobalt-Catalyzed Stereospecific C-N/C-O Bond Formation of Oxiranes with Diaziridines.

Co-catalyzed stereospecific C-N and C-O bond formation of oxiranes with diaziridines has been accomplished to furnish tetrahydro-[1,3,4]-oxadiazines at room temperature. Optically active oxiranes can be coupled with high optical purities (>96% ee). Stereoselectivity, functional group tolerance, mechanistic studies using DFT, and natural product modification are the important practical features.

Proof-of-concept studies of novel protocols for producing highly pure 48V from a 48Cr/48V generator

The quest to improve the quality of nuclear data, such as half-lives, transition yields, and reaction cross-sections, is a shared endeavor among various areas of nuclear science. 48V is a vanadium isotope for which experimental data on neutron reaction cross-sections is needed. However, traditional isotope production techniques cannot produce 48V with high enough isotopic purity for some of these measurements. “Isotope harvesting” at the Facility for Rare Isotope Beams (FRIB) is a new isotope production technique that could potentially yield 48V with the necessary purity for such studies. In this case, 48Cr would be collected and allowed to generate 48V that can be separated from undecayed 48Cr to yield highly pure 48V. Thus, any protocol for producing pure 48V via isotope harvesting would involve utilizing a separation technique that can effectively separate 48Cr and 48V. In this study, the radiotracers 51Cr and 48V were used to develop possible radiochemical separation methodologies, which can be translated to obtain high purity 48V via this novel isotope production method. The developed protocols utilize either ion exchange or extraction chromatographic resins. Separations of 51Cr and 48V with AG 1-X8 anion exchange resin respectively resulted in recoveries of 95.6(26)% and 96.2(12)% with radionuclidic purities of 92(2)% and 99(1)%. An even more effective Cr and V separation was obtained with an extraction chromatographic resin (TRU resin) and 10 M HNO3 loading solution. Here, 51Cr and 48V respectively had recoveries of 94.1(28)% and 96.2(13)% with high radionuclidic purities (100(2)% and 100(1)%) in small volumes (8.81(8) mL and 5.39(16) mL). This study suggests that, to maximize the yield and isotopic purity of 48V, the best production protocol would involve utilizing two separations with TRU resin and 10 M HNO3 to isolate 48Cr and purify the generated 48V.

Sustainable and facile process for Li2CO3 and Mn2O3 recovery from spent LiMn2O4 batteries via selective sulfation with waste copperas

Spent lithium-ion batteries (LIBs) are essential secondary resource, containing valuable metal elements including lithium, cobalt, nickel, manganese. Recovering valuable metals from spent LIBs is significant for achieving environmental protection and alleviating resource shortages. Herein, a sustainable and facile process for Li2CO3 and Mn2O3 recovery from spent LiMn2O4 batteries (LMO) was proposed via sulfation roasting with waste copperas. The leaching efficiencies of Li and Mn reached approximately 100 % and 82 % under the optimal conditions, and the final recovered products were Li2CO3 and Mn2O3 with high purities. The sulfation reaction between LMO and copperas was the transition from solid-solid to gas-solid reaction. During the sulfation reaction, LMO spinel structure was decomposed into MnO2 and Mn2O3 crystal structures, and the anti-fluorite structure Li2O embedded in the spinel structure was released. The Li2O was easily to be sulfated, while MnO2 was partly reduced by Fe2+ to more stable spinel structure Mn2O3. Furthermore, FeSO4 decomposed into SO2 gas, which greatly improved the sulfation reaction through permeating into the unreacted core of LMO. As a result, the spinel structure of Mn2O3 was broken, and Mn was escaped to combine with SO42- to form MnSO4. This research provided an alternative technological route for green recovery of spent LMO batteries, demonstrating high potential for broad application.

Optimization of 177Lu-labelling of DOTA-TOC, PSMA-I&T and FAPI-46 for clinical application

Background177Lu-radiopharmaceuticals are routinely used for the treatment of various tumor entities. The productions of radiopharmaceuticals follow strict good-manufacturing practice guidelines and synthesis optimizations thereof have a strong impact on e.g. the quality of the product, radiation safety and costs. The purpose of this study is to optimize the precursor load of three radiopharmaceuticals. For that, different precursor loads were evaluated and compared to previously reported findings.ResultsAll three radiopharmaceuticals were successfully synthesized in high radiochemical purities and yields on the ML Eazy. The precursor load was optimized for [177Lu]Lu-FAPI-46 from 27.0 to 9.7 µg/GBq, for [177Lu]Lu-DOTATOC from 11 to 10 µg/GBq and for [177Lu]Lu-PSMA-I&T from 16.3 to 11.6 µg/GBq.ConclusionsWe successfully reduced the precursor load for all three radiopharmaceuticals while maintaining their quality.

Carbene-Catalyzed Access to Thiochromene Derivatives: Control of Reaction Pathways via Slow Release of Thiols from Disulfides.

Substrates containing disulfide bonds, which are more stable and less smelling, could be used as thiophenol precursors in organic synthesis. Herein, an N-heterocyclic carbene (NHC)-catalyzed reaction between α-bromoenals and 2,2'-dithiodibenzaldehydes was developed. Through the sustained release strategy, the side reaction can be effectively inhibited, and the chiral thiochromene derivatives can be obtained with good yields and high optical purities. Application studies showed encouraging results when the desired products were explored for antimicrobial utilities in pesticide development.

Deep blue thermally activated delayed fluorescent emitters based on methyl-modified acridin-9(10H)-one acceptor

Developing deep blue thermally activated delayed fluorescence (TADF) materials with high efficiencies and good color purities is still a formidable challenge. Here, two novel deep blue TADF emitters, namely MePhCz-AD and MePhCz-AD-Py, were synthesized by incorporating two 3,6-diphenyl-9H-carbazole donors onto the methyl-modified acridin-9(10H)-one (AD) acceptor, respectively. The high rigidity of AD acceptor effectively suppressed non-radiative transition and vibration relaxation of excited states, which is favorable for a good emitting quantum yield and narrow spectral width. The presence of methyl groups at 2,7-sites of AD ring slightly reduced the acceptor strength and contributed to the deep blue emission color. Incorporation of phenyls at 3,6-sites of carbazole ring delocalized the distribution of the highest occupied molecular orbital (HOMO), promoting the radiative decay process. As a result, these two emitters showed deep blue TADF with fast radiative decay rates kR > 107 s−1. In addition, with the introduction of pyridyl (Py) group at 10-site of AD ring instead of phenyl, both the spin-orbital coupling (SOC) constant between high-lying triplet states and the lowest singlet excited state (S1) and thus the reverse intersystem crossing rate constant (kRISC) were dramatically promoted for MePhCz-AD-Py. The organic light-emitting diode with MePhCz-AD-Py as doped emitter exhibited a maximum external quantum efficiency (EQEmax) of 15.4% with a relatively narrow FWHM of 60 nm and the deep-blue color coordinates of (0.15, 0.15).

Digital Twin Based Design and Experimental Validation of a Continuous Peptide Polishing Step

Optimizing or debottlenecking existing production plants is a challenging task. In this case study, an existing reversed phased chromatography polishing step for peptide purification was optimized with the help of a digital twin. The existing batch chromatography was depicted digitally with the general rate model. Model parameter determination and model validation was done with dedicated experiments. The digital twin was then used to identify optimized process variants, especially continuous chromatography steps. MCSGP was found to achieve high purities and yield but at the cost of productivity due to column synchronization. An alternative Continuous Twin Column chromatography process (CTCC) was established that eliminates unnecessary waiting times. Ensuring the same or higher purity compared to the batch process, the continuous process achieved a yield increase of 31% and productivity increase of 27.6%. Experimental long runs confirmed these results.

Development of brain-penetrable antibody radioligands for in vivo PET imaging of amyloid-β and tau.

Alzheimer's disease (AD) is characterized by the misfolding and aggregation of two major proteins: amyloid-beta (Aβ) and tau. Antibody-based PET radioligands are desirable due to their high specificity and affinity; however, antibody uptake in the brain is limited by the blood-brain barrier (BBB). Previously, we demonstrated that antibody transport across the BBB can be facilitated through interaction with the transferrin receptor (TfR), and the bispecific antibody-based PET ligands were capable of detecting Aβ aggregates via ex vivo imaging. Since tau accumulation in the brain is more closely correlated with neuronal death and cognition, we report here our strategies to prepare four F-18-labeled specifically engineered bispecific antibody probes for the selective detection of tau and Aβ aggregates to evaluate their feasibility and specificity, particularly for in vivo PET imaging. We first created and evaluated (via both in vitro and ex vivo studies) four specifically engineered bispecific antibodies, by fusion of single-chain variable fragments (scFv) of a TfR antibody with either a full-size IgG antibody of Aβ or tau or with their respective scFv. Using [18F]SFB as the prosthetic group, all four 18F-labeled bispecific antibody probes were then prepared by conjugation of antibody and [18F]SFB in acetonitrile/0.1 M borate buffer solution (final pH ~ 8.5) with an incubation of 20 min at room temperature, followed by purification on a PD MiniTrap G-25 size exclusion gravity column. Based on both in vitro and ex vivo evaluation, the bispecific antibodies displayed much higher brain concentrations than the unmodified antibody, supporting our subsequent F18-radiolabeling. [18F]SFB was produced in high yields in 60 min (decay-corrected radiochemical yield (RCY) 46.7 ± 5.4) with radiochemical purities of >95%, confirmed by analytical high performance liquid chromatography (HPLC) and radio-TLC. Conjugation of [18F]SFB and bispecific antibodies showed a 65%-83% conversion efficiency with radiochemical purities of 95%-99% by radio-TLC. We successfully labeled four novel and specifically engineered bispecific antibodies with [18F]SFB under mild conditions with a high RCY and purities. This study provides strategies to create brain-penetrable F-18 radiolabeled antibody probes for the selective detection of tau and Aβ aggregates in the brain of transgenic AD mice via in vivo PET imaging.

Easy 250 EasySep&[trade] Magnet: A Novel Magnetic Platform For Large-Volume CD34+ Hematopoietic Stem and Progenitor Cell Isolation from Leukapheresis Products

Abstract We have developed a novel magnetic platform for large-volume CD34+ hematopoietic stem and progenitor cell (HPSC) isolation from both mobilized and non-mobilized leukapheresis products. As the frequency of CD34+ cells is low, and cell quality and viability can be variable between samples, it takes great effort to isolate these cells with consistently high purities and yields. Working with large volume leukapheresis products can be challenging as the sample often needs to be split and processed in parallel, which can be both time-consuming and labor-intensive. The Easy 250 EasySep™ Magnet simplifies cell isolation procedures when processing leukapheresis samples. It is based on column-free immunomagnetic EasySep™ cell isolation technology and can process sample volumes up to 225 mL. We have developed a negative selection protocol for the enrichment of CD34+ HPSCs (mean purity ± SD of 74.6 ± 10.5%; n = 8) from non-mobilized leukapheresis products. For mobilized leukapheresis products, an EasySep™ positive selection protocol has been optimized for the isolation of highly purified CD34+ HPSCs (mean purity ± SD of 92.0 ± 1.7%; n = 7). Notably, these protocols can be completed in as little as 25 minutes, making the Easy 250 EasySep™ Magnet the fastest and simplest method for enriching highly purified HPSCs from large-volume leukapheresis products—critical for addressing the growing clinical demands for CD34+ cell-based therapies.

Proteolytically degradable PEG hydrogel matrix mimicking tumor immune microenvironment for 3D co-culture of lung adenocarcinoma cells and macrophages

Tumor-associated macrophages and monocytes are the major stromal cell types found in the tumor immune microenvironment (TIME), which modulates tumor progression, invasion, and chemoresistance. To address the need for an in vitro three-dimensional tumor model for understanding the complex cellular interactions within the TIME, we propose a TIME-mimetic co-culture matrix composed of photo-crosslinked poly(ethylene glycol) hydrogels mimicking the characteristics of the tumor and stroma. Desmoplasia-mimetic microgels encapsulating lung adenocarcinoma cells (A549) were embedded with monocyte- or macrophage-type U937 cells in normal stroma-mimetic hydrogel, increasing the proximity between the two cell types. By modulating the proteolytic degradability of the hydrogels, we could separate different cell types with high purities for use in orthogonal assays. In addition, we demonstrated that U937 cells had distinct influences on A549 cell death depending on their activation states (i.e. monocyte, M0, or M1 phenotype). M1 macrophages suppressed tumor growth and increased the susceptibility of A549 cells to cisplatin. In contrast, monocytes upregulated cancer stem cell markers (OCT4, SOX2, and SHH) of A549 cells, showing M2-like features, such as downregulated expression of proinflammatory markers (IL6 and TNFα). These findings suggest that this co-culture system is potentially used for investigation of heterotypic cellular interactions in the TIME.

Antioxidant and Anticholinesterase Potentials of Novel 4,6-Dimethoxyindole based Unsymmetrical Azines: Synthesis, Molecular Modeling, In Silico ADME Prediction and Biological Evaluations

Chemically and biologically important -C = N-N = C- diimine linkage was used to build unsymmetrical azine systems with indole heterocyclic backbone and substituted aromatic carbaldehydes. Ten novel compounds 7a-j were synthesized by the Schiff base reaction of 4,6-dimethoxyindole-7-hydrazone 5 and a range of substituted carbaldehydes 6a-j with high yields and purities. The biological study was directed to identify the antioxidant potentials due to the expected electronic delocalization capability of designated linkage which is important for possible hydrogen or electron donation. The three different assays, namely DPPH free radical scavenging, ABTS cationic radical decolarization and CUPRAC (cupric reducing antioxidant capacity) were employed to detect the antioxidant properties. The antioxidant potentials were found to be moderate for ABTS and CUPRAC assays and the compound 7j was the most potent candidate for all the antioxidant assays. More importantly, the anticholinesterase properties were investigated by acetylcholinesterase (ACh) and butyrylcholinesterase (BCh) enzyme inhibition assays. The molecular docking studies were also carried out to determine the possible poses of ligands 7a-j in binding sites of enzymes and ligand-residue interactions. The synthesized compounds were found to be more effective for the anticholinesterase activity with three promising candidates 7d, 7h and 7j in the case of BChE inhibitions. The compound 7h was determined as the best candidate with the comparable IC50 values for AChE and better inhibition potency for BChE with 7j. A range of hydrophobic and hydrophilic interactions were detected for the designated compound 7h and 7j through different amino acid residues and the computational results were found to be compatible with the biological counterparts.