Synthetic Routes to 2-aryl-1-pyrrolo[2,3-]pyridin-4-amines: Cross-Coupling and Challenges in SEM-Deprotection.

7-Azaindoles are compounds of considerable medicinal interest. During development of the structure-activity relationship for inhibitors of the colony stimulated factor 1 receptor tyrosine kinase (CSF1R), a specific 2-aryl-1-pyrrolo[2,3-]pyridin-4-amine was needed. Two different synthetic strategies were evaluated, in which the order of the key C-C and C-N cross-coupling steps differed.

Cavity-agnostic acoustofluidic manipulations enabled by guided flexural waves on a membrane acoustic waveguide actuator.

This article presents an in-depth exploration of the acoustofluidic capabilities of guided flexural waves (GFWs) generated by a membrane acoustic waveguide actuator (MAWA). By harnessing the potential of GFWs, cavity-agnostic advanced particle manipulation functions are achieved, unlocking new avenues for microfluidic systems and lab-on-a-chip development. The localized acoustofluidic effects of GFWs arising from the evanescent nature of the acoustic fields they induce inside a liquid medium are numerically investigated to highlight their unique and promising characteristics.

Microfabricated acoustofluidic membrane acoustic waveguide actuator for highly localized in-droplet dynamic particle manipulation.

Precision manipulation techniques in microfluidics often rely on ultrasonic actuators to generate displacement and pressure fields in a liquid. However, strategies to enhance and confine the acoustofluidic forces often work against miniaturization and reproducibility in fabrication. This study presents microfabricated piezoelectric thin film membranes made silicon diffusion for guided flexural wave generation as promising acoustofluidic actuators with low frequency, voltage, and power requirements.

An Overview on Synthetic and Medicinal Perspectives of [1,2,4]Triazolo[1,5-a]pyrimidine Scaffold.

[1,2,4]Triazolo[1,5-a]pyrimidine is an important heterocyclic scaffold known to have a wide range of pharmacological activities such as anticancer, antimicrobial, anti-tubercular, CB cannabinoid agonists, feticide, and adenosine antagonists. Several clinical trials and marketed drugs such as Trapidil, Essramycin, Pyroxsulam, DSM-265, Flumetsulam, GNF-6702, and Cevipabulin indicate the potential of [1,2,4]triazolo[1,5-a]pyrimidine moiety with various functional groups in medicinal chemistry. Herein, we represent a concise report focusing on the synthetic strategies used for diversely substituted [1,2,4]triazolo[1,5-a]pyrimidine analogs and their pharmacological applications.

Development of niosomes for encapsulating captopril-quercetin prodrug to combat hypertension.

Novel and effective anti-hypertensive agents are required to manage hypertension; therefore, we synthesised a novel antihypertensive drug from captopril and quercetin (cap-que) and explored its antihypertensive potential in a niosomal formulation via molecular hybridisation. The cap-que hybrid was synthesised, and its structure was characterised via NMR, FTIR, and HRMS. Niosomes were then loaded with cap-que using the thin-film hydration method.

Novel thiomorpholine tethered isatin hydrazones as potential inhibitors of resistant Mycobacterium tuberculosis.

Novel chemotherapeutic agents against multidrug resistant-tuberculosis (MDR-TB) are urgently needed at this juncture to save the life of TB-infected patients. In this work, we have synthesized and characterized novel isatin hydrazones 4(a-o) and their thiomorpholine tethered analogues 5(a-o). All the synthesized compounds were initially screened for their anti-mycobacterial activity against the HRv strain of Mycobacterium tuberculosis (MTB) under level-I testing.

Synthesis, anticancer evaluation, and molecular docking studies of some novel 4,6-disubstituted pyrazolo[3,4-d]pyrimidines as cyclin-dependent kinase 2 (CDK2) inhibitors.

A novel series of 4,6-disubstituted pyrazolo[3,4-d]pyrimidines (7-43) bearing various anilines at C-4 position and thiophenethyl or thiopentane moieties at C-6 position have been designed and synthesized by molecular hybridization approach. All the synthesized compounds were evaluated for in vitro CDK2/cyclin E and Abl kinase inhibitory activity as well as anti-proliferative activity against K-562 (chronic myelogeneous leukemia), and MCF-7 (breast adenocarcinoma) cell lines. The structure-activity relationship (SAR) studies revealed that compounds with thiophenethyl group at C-6 with mono-substituted anilines at C-4 exhibited better CDK2 inhibitory activity compared to alkyl group (thiopentane) at C-6 and di-substituted anilines at C-4 of the scaffold.

Surface Characteristics, Biodegradability and Biocompatibility of Porous Silicon for Microfabricated Neural Electrode.

Porous Si (PSi) used for microfabrication of a novel neural electrode was prepared on Si wafers by an anodization process. Surface morphology and porous structure of the PSi were characterized using scanning electron microscopy (SEM) and transmission electron microscopy (TEM). 3D inter-connected and nano sized pores were homogeneously formed across the surface.

Telescoping intestine in an adult.

Protrusion of a bowel segment into another (intussusception) produces severe abdominal pain and culminates in intestinal obstruction. In adults, intestinal obstruction due to intussusception is relatively rare phenomenon, as it accounts for minority of intestinal obstructions in this population demographic. Organic lesion is usually identifiable as the cause of adult intussusceptions, neoplasms account for the majority.

Plasma-assisted atomic layer deposition of Al(2)O(3) and parylene C bi-layer encapsulation for chronic implantable electronics.

Encapsulation of biomedical implants with complex three dimensional geometries is one of the greatest challenges achieving long-term functionality and stability. This report presents an encapsulation scheme that combines Al(2)O(3) by atomic layer deposition with parylene C for implantable electronic systems. The Al(2)O(3)-parylene C bi-layer was used to encapsulate interdigitated electrodes, which were tested invitro by soak testing in phosphate buffered saline solution at body temperature (37 °C) and elevated temperatures (57 °C and 67 °C) for accelerated lifetime testing up to 5 months.

Characterization of polymerized liposomes using a combination of dc and cyclical electrical field-flow fractionation.

Characterization of polymerized liposomes (PolyPIPosomes) was carried out using a combination of normal dc electrical field-flow fractionation and cyclical electrical field-flow fractionation (CyElFFF) as an analytical technique. The constant nature of the carrier fluid and channel configuration for this technique eliminates many variables associated with multidimensional analysis. CyElFFF uses an oscillating field to induce separation and is performed in the same channel as standard dc electrical field-flow fractionation separation.

Diffusion Split-Flow Thin Cell (SPLITT) system for protein separations.

A diffusion Split-Flow Thin Cell (SPLITT) system was used to partially remove small peptides such as β2 microglobulin (β2M) and parathyroid hormone (PTH) in a continuous manner from an input flow stream while preserving most (over 97%) of the larger protein in the sample, such as albumin. To help determine the operating conditions for this work, a two-dimensional numerical model based on the Navier-Stokes equation and convection-diffusion equations was developed for diffusional SPLITT using COMSOL multiphysics software (COMSOL Inc., MA).

A novel method for effective field measurements in electrical field-flow fractionation.

The electric field that drives separation and retention in electrical field flow fractionation (ElFFF) and cyclical electrical field-flow fractionation (CyElFFF) is a complex function of many parameters such as carrier ionic strength and pH, voltage, channel dimensions, flowrate, and electrode material. Currently there is no accurate or in situ method to measure the field during system operation. This paper introduces a technique to measure the effective electric field during ElFFF and CyElFFF operation using transient electrical spikes.

Interaction of silver nanoparticles with an environmentally beneficial bacterium, Pseudomonas chlororaphis.

This study explores the potential antimicrobial mechanisms of commercial silver nanoparticles (Ag NPs) in the environmental bacterium, Pseudomonas chlororaphis O6. The 10nm size NPs aggregated in water, as demonstrated by atomic force microscopy. Solubility of the NPs at 10mg/L was 0.

Optimization of cyclical electrical field flow fractionation.

Cyclical electrical field flow fractionation (CyElFFF) is a variation on electrical field flow fractionation (ElFFF) where cyclical electrical fields are used instead of steady DC fields to increase the effective field experienced by particles in the flow channel. Even though the effective field increases more than 20-fold compared to normal ElFFF, the retention and resolution in CyElFFF has not been shown to be better than in ElFFF. In this paper we report how one can optimize operational parameters in CyElFFF to obtain good retention and resolution in CyElFFF.

Mutational analysis of the eyeless gene and phenotypic rescue reveal that an intact Eyeless protein is necessary for normal eye and brain development in Drosophila.

Pax6 genes encode evolutionarily highly conserved transcription factors that are required for eye and brain development. Despite the characterization of mutations in Pax6 homologs in a range of organisms, and despite functional studies, it remains unclear what the relative importance is of the various parts of the Pax6 protein. To address this, we have studied the Drosophila Pax6 homolog eyeless.

Vitamin D status before Roux-en-Y and efficacy of prophylactic and therapeutic doses of vitamin D in patients after Roux-en-Y gastric bypass surgery.

Background: Literature regarding the effect of Roux-en-Y gastric bypass (RYGBP) on vitamin D level shows contradictory findings. Our goal was to determine preoperatively vitamin D levels, to evaluate the efficacy of therapeutic and prophylactic doses of vitamin D and to assess the relationship of 25-OH vitamin D level and body mass index (BMI).

Methods: We conducted a retrospective cross-sectional study of 72 patients who underwent RYGBP from April 2007 to October 2007 in Bariatric Surgery Department at Saint Vincent Charity Hospital.

Improved theory of cyclical electrical field flow fractionation.

Previously reported theories for cyclical electrical field flow fractionation (CyElFFF) are severely limited in that they do not account for diffusion, steric, or electric double layer effects. Experiments have shown that these theories overpredict the retention of particles in CyElFFF. In this work, we present a model for prediction of steric, diffusion, and electrical effects.

Characterization of a microscale cyclical electrical field flow fractionation system.

A microscale cyclical electrical field flow fractionation (CyElFFF) channel is characterized with regard to the effect of various operating parameters and comparison made to recent theoretical developments. Challenges associated with various operating conditions are reported along with some of the optimized operating parameters. The effect of retention wall choice, an offset voltage, relaxation steps, and flow rates, along with the basic operating parameters of voltage, frequency, and electrophoretic mobility are reported.

Effect of carrier ionic strength in microscale cyclical electrical field-flow fractionation.

Recent work with cyclical electrical field-flow fractionation systems has shown promise for the technique as a separation and analysis tool, but little is understood about how the carrier composition in the system affects its capabilities. The electrical properties of microscale CyElFFF systems change when the carrier ionic conditions are altered, and it is well known that the effects of increasing ionic strength carriers on retention in normal ElFFF systems are severe. Specifically, retention levels fall significantly.

Cyclical electrical field flow fractionation.

Cyclical electrical field flow fractionation (Cy/ElFFF) is demonstrated in a standard electrical field flow fractionation (ElFFF) channel for the first time. Motivation for the use of alternating current (AC) fields in a traditionally direct current (DC) technique are discussed. The function of the system over a wide range of operating conditions is explored and challenges associated with various operating conditions reported.