Background/Objectives: The principal aim of this work was to prepare a liposomal drug delivery system based on the commercial doxorubicin (DOX) and budding agent with promising anticancer activity, 9-(N-piperazinyl)-5-methyl-12(H)-quino [3,4-b][1,4]benzothiazinium chloride (9-PBThACl). Methods: A spectrophotometric methodology used meticulously investigate entrapment release characteristics new complexes (L) dipalmitoylphosphatidylcholine (DPPC) human serum albumin (HSA) its defeated analog...

In the study, a series of twelve ring-substituted 4-hydroxy-1H-quinolin-2-one derivatives were prepared. The procedures for synthesis compounds are presented. analyzed using RP-HPLC to determine lipophilicity and tested their photosynthesis-inhibiting activity spinach (Spinacia oleracea L.) chloroplasts. All synthesized also evaluated antifungal in vitro screening with eight fungal strains. For all compounds, relationships between chemical structure studied discussed, as well...

A novel and selective sorbent for micro-solid phase extraction was synthesized by chemical functionalization of graphene oxide with glycine.

The sulfur-containing derivatives and their metabolites, regarded as ‘old devils of green’ chemistry, constitute a relevant class air/water/soil contaminants in over-polluted world. In fact, some industrially-engineered solvents have become environmentally unfavorable. An attractive alternative to commonly used industrial liquids is sulfolane (C4H8SO2), an anthropogenic medium. main objective this paper the comprehensive review focusing mainly on state-of-the-art aspects synthesis,...

The potential implementation of Envifer®, a commercial product containing potassium ferrate (40.1% K2FeO4), for the purification highly contaminated tannery wastewater from leather dyeing processes was proposed. employment Taguchi method optimization experiments allowed discoloration (98.4%), chemical oxygen demand (77.2%), total organic carbon (75.7%), and suspended solids (96.9%) values to be lowered using 1.200 g/L K2FeO4 at pH 3 within 9 min. application central composite design (CCD)...

An attempt was made to estimate the annual production of CH4 at a municipal waste landfill site in Poland. As matter fact, extent unorganized emission from surface approached based on adopted mathematical model. The Ward agglomeration method for cluster analysis and Pearson coefficient were employed evaluate distance-based similarity measure optimize methods estimating methane emissions as well verify input parameters In order calculate content biodegradable organic parts waste,...

The synthesis and application of sodium trithiocarbonate (Na2CS3) for the treatment real galvanic wastewater in order to remove heavy metals (Cu, Cd Zn) was investigated. A Central Composite Design/Response Surface Methodology (CCD/RSM) employed optimize removal from industrial wastewater. Adequacy approximated data verified using Analysis Variance (ANOVA). calculated coefficients determination (R2 R2adj) were 0.9119 0.8532, respectively. Application Na2CS3 conjugated with CCD/RSM allowed...

Determining the properties of nanoparticles obtained by novel methods and defining scope their application as drug carriers has important practical significance. This article presents pioneering studies concerning high degree incorporation cytarabine (AraC) methotrexate (MTX) into liposome vesicles. The main focus this study were cytarabine-methotrexate-dipalmitoylphosphatidylcholine (DPPC) interactions observed in gel fluid phases DPPC bilayers. proposed new method use...

A library of novel 4-{[(benzyloxy)carbonyl]amino}-2-hydroxybenzoic acid amides was designed and synthesized in order to provide potential acetyl- butyrylcholinesterase (AChE/BChE) inhibitors; the vitro inhibitory profile selectivity index were specified. Benzyl(3-hydroxy-4-{[2-(trifluoromethoxy)phenyl]carbamoyl}phenyl)carbamate best AChE inhibitor with concentration IC50 = 36.05 µM series, while benzyl{3-hydroxy-4-[(2-methoxyphenyl)carbamoyl]phenyl}-carbamate most potent BChE (IC50 22.23 µM)...

Pancreatic ductal adenocarcinoma (PDAC) is a weakly immunogenic fatal neoplasm. Oncolytic viruses with dual anti-cancer properties—oncolytic and immune response-boosting effects—have great potential for PDAC management. Adipose-derived stem cells (ADSCs) of mesenchymal origin were infected ex vivo recombinant myxoma virus (MYXV), which encodes murine LIGHT, also called tumor necrosis factor ligand superfamily member 14 (TNFSF14). The viability proliferation ADSCs not remarkably decreased...

The aim of this study is to prepare a liposomal delivery system for 5-methyl-12 (H)-quino[3,4-b]-1,4-benzothiazine chloride (5-MBT) and the in vitro release characteristics. 5-MBT from complex with human serum albumin (HSA) [LDPPC/5-MBT]:HSA was examined using spectrophotometric method differential scanning calorimetry (DSC). Electronic paramagnetic resonance used assess influence pH environment on conformation phospholipids, latter determining degree encapsulated compound. applied...

A hybrid approach that combines 3D and 4D-QSAR methods based on grid neural paradigms with automated IVE-PLS procedure was examined to identify the pharmacophore pattern for cholic acid derivatives as potential drug absorption promoters.

The antitumor potency of a series designed and prepared antibacterial quinobenzothiazines was evaluated against different types human cancer cell lines, such as glioblastoma SNB-19, lung adenocarcinoma A549 breast T47D, the activities compounds were compared to cisplatin doxorubicin. 9-Propoxy-5-methyl-12H-quino[3,4-b][1,4]benzo- thiazinium chloride (4a), 9-allyloxy-5-methyl-12H-quino[3,4-b][1,4]benzothiazinium (4d) 11-benzyloxy-5-methyl-12H-quino[3,4-b][1,4]benzothiazinium (4l) most active...

Series of twenty-five benzyl (2S)-2-(arylcarbamoyl)pyrrolidine-1-carboxylates was prepared and completely characterized. All the compounds were tested for their in vitro ability to inhibit acetylcholinesterase (AChE) butyrylcholinesterase (BChE), selectivity individual cholinesterases determined. Screening cytotoxicity all performed using a human monocytic leukaemia THP-1 cell line, demonstrated insignificant toxicity. showed rather moderate inhibitory effect against AChE;...

A series of twenty-six methoxylated and methylated N-aryl-1-hydroxynaphthalene- 2-carboxanilides was prepared characterized as potential anti-invasive agents. The molecular structure N-(2,5-dimethylphenyl)-1-hydroxynaphthalene-2-carboxamide a model compound determined by single-crystal X-ray diffraction. All the analysed compounds were tested against reference strain Staphylococcus aureus three clinical isolates methicillin-resistant S. well Mycobacterium tuberculosis M. kansasii. In...

A series of new benzene-based derivatives was designed, synthesized and comprehensively characterized. All the tested compounds were evaluated for their in vitro ability to potentially inhibit acetyl- butyrylcholinesterase enzymes. The selectivity index individual molecules cholinesterases also determined. Generally, inhibitory potency stronger against butyryl- compared acetylcholinesterase; however, some showed a promising inhibition both In fact, two (23, benzyl...

Chemically functionalized graphene oxides could be used as novel drug carriers. Covalent alterations of lead to surface changes via formation chemical bonding while non-covalent ones involve van der Waals forces, hydrogen bonding, and π-π stacking interactions. modifications appear superior they can yield compounds with desired properties carriers prepared by other methods are less stable. Synthesis oxide-iminodiacetic acid oxide-glycine involves nucleophilic substitution oxide nanoparticles...

Finding a balance between desired drug's potency and its physicochemical properties that are important for molecule pharmacokinetic or pharmacodynamics profile is still challenging issue in rational drug discovery. Quantitative assessment of the lipophilic characteristics potential molecules indispensable efficient development Absorption, Distribution, Metabolism, Excretion, Toxicity-tailored structure–activity models; therefore reliable procedures deriving log P from molecular structure...

In this paper, we describe a new method for synthesizing hybrid combinations of 1,2,3-triazoles with tetracyclic quinobenzothiazinium system. The developed approach allowed the production series azaphenothiazine derivatives 1,2,3-triazole system in different positions benzene ring. practice, methodology consists reaction triazole aniline thioquinanthrenediinium bis-chloride. structure products was determined by 1H-NMR, 13C-NMR spectroscopy, and HR-MS spectrometry, respectively. Moreover,...

A series of twenty-two novel N-(disubstituted-phenyl)-3-hydroxynaphthalene- 2-carboxamide derivatives was synthesized and characterized as potential antimicrobial agents. N-[3,5-bis(trifluoromethyl)phenyl]- N-[2-chloro-5-(trifluoromethyl)phenyl]-3-hydroxy- naphthalene-2-carboxamide showed submicromolar (MICs 0.16–0.68 µM) activity against methicillin-resistant Staphylococcus aureus isolates. N-[4-bromo-3-(trifluoromethyl)phenyl]-3-hydroxynaphthalene-2-carboxamide revealed M. tuberculosis...

The evaluation of the lipophilic characteristics biologically active agents is indispensable for rational design ADMET-tailored structure–activity models. N-Alkoxy-3-hydroxynaphthalene-2-carboxanilides, N-alkoxy-1-hydroxynaphthalene-2-carboxanilides, and N-alkoxy-2-hydroxynaphthalene-1-carboxanilides were recently reported as a series compounds with antimycobacterial, antibacterial, herbicidal activity. As it was found that lipophilicity these determines their activity, hydro-lipophilic...