Random poly(ε‐caprolactone‐L‐alanine) by direct melt copolymerization

A series of random polyesteramides (PEAs) with a range of molar composition from 90/10 to 50/50 were synthesized by direct melt polycondensation of ε‐caprolactone and l ‐alanine. Their structure was fully characterized by Fourier transform IR and NMR spectroscopy. The resulting copolymers are completely amorphous with the exception of PEA‐90/10 which possesses a semicrystalline structure. These PEAs present increasing glass transition temperatures at increasing l ‐alanine contents and exhibit fairly good thermal stability with 10% mass loss temperatures reaching 315 °C. © 2020 Society of Industrial Chemistry     

Steward: Scaling Byzantine Fault-Tolerant Replication to Wide Area Networks

This paper presents the first hierarchical Byzantine fault-tolerant replication architecture suitable to systems that span multiple wide-area sites. The architecture confines the effects of any malicious replica to its local site, reduces message complexity of wide-area communication, and allows read-only queries to be performed locally within a site for the price of additional standard hardware. We present proofs that our algorithm provides safety and liveness properties. A prototype implementation is evaluated over several network topologies and is compared with a flat Byzantine fault-tolerant approach. The experimental results show considerable improvement over flat Byzantine replication algorithms, bringing the performance of Byzantine replication closer to existing benign fault-tolerant replication techniques over wide area networks.     

Control Systems on Three-Dimensional Lie Groups: Equivalence and Controllability

We consider left-invariant control affine systems, evolving on three-dimensional matrix Lie groups. Equivalence and controllability are investigated. All full-rank systems are classified, under detached feedback equivalence. A representative is identified for each equivalence class. The controllability nature of these representatives is determined.     

Selenocarbamates As a Prodrug-Based Approach to Carbonic Anhydrase Inhibition

A study on the activity of selenocarbamates as a novel chemotype acting as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors is reported. Undergoing CA-mediated hydrolysis, selenocarbamates release selenolates behaving as zinc binding groups and effectively inhibiting CAs. A series of selenocarbamates characterised by high molecular diversity and complexity have been studied against different human CA isoforms such as hCA I, II, IX and XII. Selenocarbamates behave as masked selenols with potential biological applications as prodrugs for CAs inhibition-based strategies. X-ray studies provided insights into the binding mode of this novel class of CA inhibitors.     

Synthesis,structural and morphological characteristics,magnetic and optical properties of Co doped ZnO nanoparticles

Zn_1−xCo_xO (x==0.05, 0.10, 0.15) nanoparticles have been synthesized by an alternative wet-chemical synthesis route using the SimAdd technique. The as-obtained powders were investigated by FT-IR spectroscopy, X-ray diffraction and thermal analysis correlated with evolved gas analysis (TG–DTA–FT-IR) in order to determine their chemical nature, crystalline structure and to establish the decomposition sequences. The precipitates are generally amorphous, but low-intensity reflection peaks assigned both to the zinc oxalate dihydrate, and zinc hydroxide can be observed in the recorded patterns, indicating that hydroxy-oxalate precipitates were obtained. The structure, morphology and magnetic properties of the thermally treated samples have been investigated by X-ray diffraction, FT-IR, HRTEM, SAED, UV–vis and EPR. XRD studies reveal a hexagonal wurtzite-type structure for all Zn_1−xCo_xO samples. TEM investigations show particle size between 28 and 37 nm, with spherical and polyhedral shapes and with tendency to form aggregates. The presence of a Co₃O₄ secondary phase was evidenced by XRD, UV–vis and EPR for the Zn_0.85Co_0.15O sample. The ferromagnetic behavior of the samples was revealed. The paper highlights that by varying the cobalt concentration it is possible to modulate the structural, morphological, optical and magnetic properties.     

Novel 1,3,5-Triazinyl Aminobenzenesulfonamides Incorporating Aminoalcohol,Aminochalcone and Aminostilbene Structural Motifs as Potent Anti-VRE Agents,and Carbonic Anhydrases I,II, VII,IX, and XII Inhibitors

A series of 1,3,5-triazinyl aminobenzenesulfonamides substituted by aminoalcohol, aminostilbene, and aminochalcone structural motifs was synthesized as potential human carbonic anhydrase (hCA) inhibitors. The compounds were evaluated on their inhibition of tumor-associated hCA IX and hCA XII, hCA VII isoenzyme present in the brain, and physiologically important hCA I and hCA II. While the test compounds had only a negligible effect on physiologically important isoenzymes, many of the studied compounds significantly affected the hCA IX isoenzyme. Several compounds showed activity against hCA XII; (E)-4-{2-[(4-[(2,3-dihydroxypropyl)amino]-6-[(4-styrylphenyl)amino]-1,3,5-triazin-2-yl)amino]ethyl}benzenesulfonamide (31) and (E)-4-{2-[(4-[(4-hydroxyphenyl)amino]-6-[(4-styrylphenyl)amino]-1,3,5-triazin-2-yl)amino]ethyl}benzenesulfonamide (32) were the most effective inhibitors with K_Is = 4.4 and 5.9 nM, respectively. In addition, the compounds were tested against vancomycin-resistant Enterococcus faecalis (VRE) isolates. (E)-4-[2-({4-[(4-cinnamoylphenyl)amino]-6-[(4-hydroxyphenyl)amino]-1,3,5-triazin-2-yl}amino)ethyl]benzenesulfonamide (21) (MIC = 26.33 µM) and derivative 32 (MIC range 13.80–55.20 µM) demonstrated the highest activity against all tested strains. The most active compounds were evaluated for their cytotoxicity against the Human Colorectal Tumor Cell Line (HCT116 p53 +/+). Only 4,4’-[(6-chloro-1,3,5-triazin-2,4-diyl)bis(iminomethylene)]dibenzenesulfonamide (7) and compound 32 demonstrated an IC₅₀ of ca. 6.5 μM; otherwise, the other selected derivatives did not show toxicity at concentrations up to 50 µM. The molecular modeling and docking of active compounds into various hCA isoenzymes, including bacterial carbonic anhydrase, specifically α-CA present in VRE, was performed to try to outline a possible mechanism of selective anti-VRE activity.     

Synthesis,Computational Studies and Assessment of in Vitro Activity of Squalene Derivatives as Carbonic Anhydrase Inhibitors

We report novel molecules incorporating the nontoxic squalene scaffold and different carbonic anhydrase inhibitors (CAIs). Potent inhibitory action, in the low-nanomolar range, was detected against isoforms hCA II for sulfonamide derivatives, which proved to be selective against this isoform over the tumor-associate hCA IX and XII isoforms. On the other hand, coumarin derivatives showed weak potency but high selectivity against the tumor-associated isoform CA IX. These compounds are interesting candidates for preclinical evaluation in glaucoma or various tumors in which the two enzymes are involved. In addition, an in silico study of inhibitor-bound hCA II revealed extensive interactions with the hydrophobic pocket of the active site and provided molecular insights into the binding properties of these new inhibitors.     

Sorption/release of diclofenac sodium in/from free‐standing poly(acrylic acid)/poly(ethyleneimine) multilayer films

Polyelectrolyte multilayer films deposited onto various substrates have been used extensively as drug delivery systems. However, little attention has been paid to the release of drugs from free‐standing polymeric films. Herein, we report the construction of thermal crosslinked free‐standing poly(acrylic acid) (PAA)/branched poly(ethyleneimine) (PEI) multilayer films composed of 25 double layers [(PAA/PEI)₂₅] and their use in sorption/release of diclofenac sodium (DS). The (PAA/PEI)₂₅ multilayer films were characterized by scanning electron microscopy, potentiometric titrations and Fourier transform infrared spectroscopy, while the sorption/release of DS was monitored by UV – Vis spectroscopy. The DS sorption equilibrium data were fitted with five isotherm models (Langmuir, Freundlich, Sips, Dubinin–Radushkevich, and Temkin). The maximum equilibrium sorption capacity, q_m, given by the Langmuir model was 32.42 mg DS/g. The Korsmeyer–Peppas semiempirical equation showed that the release of DS from the free‐standing (PAA/PEI)₂₅ films proceeded by pseudo‐Fickian diffusion, irrespective of the releasing media. © 2016 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2016 , 133, 43752.     

Water-Based Graphene Oxide–Silicon Hybrid Nanofluids—Experimental and Theoretical Approach

In the current paper, a new hybrid nanofluid based on graphene oxide sheets and silicon nanoparticles is proposed for thermal applications. GO sheets and Si nanoparticles with different mixture ratios are dispersed in distilled water. Dynamic viscosity is measured at temperatures within the range 20–50 °C and the values are compared to the results available in the literature. The results indicated that the viscosity increases with increasing the mixture ratio of graphene oxide. A new correlation for the dynamic viscosity based on the experimental findings is proposed. Finally, the criteria for the performance of new hybrid nanofluid for thermal applications are analyzed.