Synthesis of 10-Hydroxycamptothecin: Evaluation of New Moderators for the Chemoselective Reduction of Camptothecin

Abstract

10-Hydroxycamptothecin is prepared by chemoselective catalytic hydrogenation of the B-ring of camptothecin over PtO₂ with sulfur moderators followed by oxidation using iodobenzenediacetate. New moderators (viz. thioanisole, dimethyl sulfide, diphenyl sulfide, 2-mercapto ethanol), which moderate the hydrogenation of the B- ring of camptothecin, are being explored.

Synthesis of N-Acyl Triazolyl-Pyrazolines via Acylation Initiated by the Hydrazone Moiety with Carboxylic Acids

An efficient synthesis of N-acyl/N-substituted acyl pyrazolines and their triazole hybrids have been accomplished via acylation of pyrazolines and pyrazoline-triazole hybrids with carboxylic acids and/or substituted carboxylic acids in the absence of activating agents/catalysts. In the present study, a mechanism envisaging the in situ generation of a new transient acylating intermediate has been proposed to explain the acylation.     

Design and In Vitro Evaluation of Solid-Lipid Nanoparticle Drug Delivery for Aceclofenac

Solid-lipid nanoparticles (SLNs) are an interesting nanoparticulate delivery system. The present work was carried out with the aim to develop a prolonged release solid-lipid nanoparticulate system for the drug using aceclofenac. Aceclofenac-loaded solid-lipid nanoparticles (ACSLNs) was prepared by hot high pressure homogenization technique. Tripalmitin was used as the lipid core. Surfactants (Poloxamer 188, Tween 80, and soya lecithin) and co-surfactant (sodium tauro glycholate) were used in the formulations. The prepared ACSLN formulations were characterized for encapsulation efficiency (EE), photon correlation spectroscopy (PCS), scanning electron microscopy (SEM), and x-ray diffraction (XRD). From these studies, mean particle diameter of the formulation prepared with combination of surfactants (Poloxmer 188 and Tween 80) was about 200 nm with spherical morphology and amorphous nature. Higher EE was obtained with SLNs prepared using combination of soya lecithin and poloxmer 188. The organization and distribution of the ingredients in the nanoparticulate system were studied by differential scanning calorimetry (DSC) and the results showed that the drug is incorporated into the solid matrix. The prepared formulations demonstrated favorable in vitro prolonged release characteristics. Experimental in vitro release data were substituted in available mathematical models to establish the release kinetics of ACSLNs and it was found to follow first-order kinetics and Higuchi diffusion mechanism. Our results suggest that these SLN formulations could constitute a promising approach for the drug delivery of aceclofenac.     

Influence of sputter power on structural and electrical properties of TiO2 films for Al/TiO2/Si gate capacitors

Titanium dioxide (TiO₂) thin films were deposited onto p‐Si substrates held at room temperature by reactive Direct Current (DC) magnetron sputtering at various sputter powers in the range 80–200 W. The as‐deposited TiO₂ films were annealed at a temperature of 1023 K. The post‐annealed films were characterized for crystallographic structure, chemical binding configuration, surface morphology and optical absorption. The electrical and dielectric properties of Al/TiO₂/p‐Si structure were determined from the capacitance–voltage and current–voltage characteristics. X‐ray diffraction studies confirmed that the as‐deposited films were amorphous in nature. After post‐annealing at 1023 K, the films formed at lower powers exhibited anatase phase, where as those deposited at sputter powers > 160 W showed the mixed anatase and rutile phases of TiO₂. The surface morphology of the films varied significantly with the increase of sputter power. The electrical and dielectric properties on the air‐annealed Al/TiO₂/p‐Si structures were studied. The effect of sputter power on the electrical and dielectric characteristics of the structure of Al/TiO₂/p‐Si (metal‐insulator‐semiconductor) was systematically investigated. Copyright © 2014 John Wiley & Sons, Ltd.     

Aliphatic Amine Discrimination by Pentafluorophenyl Dibromo BODIPY

Two new fluorescent BODIPY dyes have been designed and synthesized. They dyes differ in their meso substituents, which have different electronic properties. Their selective reactivity towards an Ar‐S_N2 reaction has been explored as a potential basis for colorimetric and fluorescent discrimination of primary, secondary and tertiary aliphatic amines. This dual‐mode, instantaneous recognition event is unprecedented.     

Electrochemical biosensors based on Ti3C2Tx MXene: future perspectives for on-site analysis

MXenes are recently developed two-dimensional layered materials composed of early transition metal carbides and/or nitrides that provide unique characteristics for biosensor applications. This review presents the recent progress made on the usage and applications of MXenes in the field of electrochemical biosensors, including microfluidic biosensors and wearable microfluidic biosensors, and highlights the challenges with possible solutions and future needs. The multilayered configuration and high conductivity make these materials as an immobilization matrix for the biomolecule immobilization with activity retention and to be explored in the fabrication of electrochemical sensors, respectively. First, how the MXene nanocomposite as an electrode modifier affects the sensing performance of the electrochemical biosensors based on enzymes, aptamer/DNA, and immunoassays is well described. Second, recent developments in MXene nanocomposites as wearable biosensing platforms for the biomolecule detection are highlighted. This review pointed out the future concerns and directions for the use of MXene nanocomposites to fabricate advanced electrochemical biosensors with high sensitivity and selectivity. Specifically, possibilities for developing microfluidic electrochemical sensors and wearable electrochemical microfluidic sensors with integrated biomolecule detection are emphasized.     

Approaches for Mitigating Microbial Biofilm-Related Drug Resistance: A Focus on Micro- and Nanotechnologies

Biofilms play an essential role in chronic and healthcare-associated infections and are more resistant to antimicrobials compared to their planktonic counterparts due to their (1) physiological state, (2) cell density, (3) quorum sensing abilities, (4) presence of extracellular matrix, (5) upregulation of drug efflux pumps, (6) point mutation and overexpression of resistance genes, and (7) presence of persister cells. The genes involved and their implications in antimicrobial resistance are well defined for bacterial biofilms but are understudied in fungal biofilms. Potential therapeutics for biofilm mitigation that have been reported include (1) antimicrobial photodynamic therapy, (2) antimicrobial lock therapy, (3) antimicrobial peptides, (4) electrical methods, and (5) antimicrobial coatings. These approaches exhibit promising characteristics for addressing the impending crisis of antimicrobial resistance (AMR). Recently, advances in the micro- and nanotechnology field have propelled the development of novel biomaterials and approaches to combat biofilms either independently, in combination or as antimicrobial delivery systems. In this review, we will summarize the general principles of clinically important microbial biofilm formation with a focus on fungal biofilms. We will delve into the details of some novel micro- and nanotechnology approaches that have been developed to combat biofilms and the possibility of utilizing them in a clinical setting.     

Structural and magnetic studies on spark plasma sintered SmCo5/Fe bulk nanocomposite magnets

SmCo₅+x wt% Fe (x=0$x=0$, 5 and 10) nanocomposite powders were synthesized by mechanical milling and were consolidated into bulk shape by spark plasma sintering (SPS) technique. The evolution of structure and magnetic properties were systematically investigated in milled powders as well as in SPS samples. A maximum coercivity of 8.9 kOe was achieved in spark plasma sintered SmCo₅+5 wt% Fe sample. The exchange spring interaction between the hard and soft magnetic phases was evaluated using δM–H measurements and the analysis revealed that the SPS sample containing 5 wt% Fe had a stronger exchange coupling between the magnetic phases than that of the sample with10 wt% Fe.     

Electrokinetic actuation of an uncharged polarizable dielectric droplet in charged hydrogel medium

Electrokinetic transport of an uncharged nonconducting microsized liquid droplet in a charged hydrogel medium is studied. Dielectric polarization of the liquid drop under the action of an externally imposed electric field induces a non-homogeneous charge density at the droplet surface. The interactions of the induced surface charge of the droplet with the immobile charges of the hydrogel medium generates an electric force to the droplet, which actuates the drop through the charged hydrogel medium. A numerical study based on the first principle of electrokinetics is adopted. Dependence of the droplet velocity on its dielectric permittivity, bulk ionic concentration, and immobile charge density of the gel is analyzed. The surface conduction is significant in presence of charged gel, which creates a concentration polarization. The impact of the counterion saturation in the Debye layer due to the dielectric decrement of the medium is addressed. The modified Nernst–Planck equation for ion transport and the Poisson equation for the electric field is considered to take into account the dielectric polarization. A quadrupolar vortex around the uncharged droplet is observed when the gel medium is considered to be uncharged, which is similar to the induced charge electroosmosis around an uncharged dielectric colloid in free-solution. We find that the induced charge electrokinetic mechanism creates a strong recirculation of liquid within the droplet and the translational velocity of the droplet strongly depends on its size for the dielectric droplet embedded in a charged gel medium.     

Irradiation of Fe–Mn@SiO2 with microwave energy enhanced its Fenton-like catalytic activity for the degradation of methylene blue

Research on Chemical Intermediates - The application of microwave energy in the synthesis of catalytic materials has been indicated to induce desirable effects that lead to improved activity....