An Update on Synthesis of Coumarin Sulfonamides as Enzyme Inhibitors and Anticancer Agents

Coumarin is an important six-membered aromatic heterocyclic pharmacophore, widely distributed in natural products and synthetic molecules. The versatile and unique features of coumarin nucleus, in combination with privileged sulfonamide moiety, have enhanced the broad spectrum of biological activities. The research and development of coumarin, sulfonamide-based pharmacology, and medicinal chemistry have become active topics, and attracted the attention of medicinal chemists, pharmacists, and synthetic chemists. Coumarin sulfonamide compounds and analogs as clinical drugs have been used to cure various diseases with high therapeutic potency, which have shown their enormous development value. The diversified and wide array of biological activities such as anticancer, antibacterial, anti-fungal, antioxidant and anti-viral, etc. were displayed by diversified coumarin sulfonamides. The present systematic and comprehensive review in the current developments of synthesis and the medicinal chemistry of coumarin sulfonamide-based scaffolds give a whole range of therapeutics, especially in the field of oncology and carbonic anhydrase inhibitors. In the present review, various synthetic approaches, strategies, and methodologies involving effect of catalysts, the change of substrates, and the employment of various synthetic reaction conditions to obtain high yields is cited.     

On the completeness of eigenfunctions of the Frankl problem with the oddness condition

Modified Frankl problems with the oddness condition are considered for the Lavrent’ev-Bitsadze equation. The eigenvalues and eigenfunctions of these problems are found. The completeness of these eigenfunctions in the elliptic part of the domain is proved.     

Experimental Study of Effect of Temperature Variations on the Impedance Signature of PZT Sensors for Fatigue Crack Detection

Structural health monitoring (SHM) is recognized as an efficient tool to interpret the reliability of a wide variety of infrastructures. To identify the structural abnormality by utilizing the electromechanical coupling property of piezoelectric transducers, the electromechanical impedance (EMI) approach is preferred. However, in real-time SHM applications, the monitored structure is exposed to several varying environmental and operating conditions (EOCs). The previous study has recognized the temperature variations as one of the serious EOCs that affect the optimal performance of the damage inspection process. In this framework, an experimental setup is developed in current research to identify the presence of fatigue crack in stainless steel (304) beam using EMI approach and estimate the effect of temperature variations on the electrical impedance of the piezoelectric sensors. A regular series of experiments are executed in a controlled temperature environment (25°C–160°C) using 202 V1 Constant Temperature Drying Oven Chamber (Q/TBXR20-2005). It has been observed that the dielectric constant ε₃₃^T which is recognized as the temperature-dependent constant of PZT sensor has sufficiently influenced the electrical impedance signature. Moreover, the effective frequency shift (EFS) approach is optimized in term of significant temperature compensation for the current impedance signature of PZT sensor relative to the reference signature at the extended frequency bandwidth of the developed measurement system with better outcomes as compared to the previous literature work. Hence, the current study also deals efficiently with the critical issue of the width of the frequency band for temperature compensation based on the frequency shift in SHM. The results of the experimental study demonstrate that the proposed methodology is qualified for the damage inspection in real-time monitoring applications under the temperature variations. It is capable to exclude one of the major reasons of false fault diagnosis by compensating the consequence of elevated temperature at extended frequency bandwidth in SHM.     

Ultrasensitive Simultaneous Quantification of Nanomolar Level of Cd and Zn by Cathodic Adsorptive Stripping Voltammetry in Some Real Samples

A novel, simple and sensitive adsorptive stripping voltammetry method was developed for simultaneous determination of Cd and Zn using N‐Nitrozo‐N‐phenylhydroxylamine (Cupferron) as a selective complexing agent. Cadmium and zinc metals gave peaks that were distinctly separated by 450–1200 mV, allowing their determination over a wide range of concentrations. The influence of pH and the nature of supporting electrolytes, concentration of ligand, preconcentration time and applied potential were investigated. The detection limits were 0.058 ng/mL for Zn and 0.092 ng/mL for Cd, and the RSD at a concentration level of 50 ppb, were 1.8–2.1 % for both zinc and cadmium, respectively. The method was applied to the determination of cadmium and zinc in blood, drug, food and water samples with the satisfactory results.     

New Guaipyridine Sesquiterpene Alkaloids from Artemisia rupestris L.

Three new guaipyridine sesquiterpene alkaloids, rupestine A, B, C ( 1 – 3 , resp.), and the new nor‐sesquiterpne alkaloid rupestine D ( 4 ) were obtained from the flowers of Artemisia rupestris L. Their structures were elucidated on the basis of sepectroscopic data and by comparison with those of the related compounds reported in the literature. In addition, the absolute configurations of 2 and 4 were determined by single‐crystal X‐ray diffraction analyses.     

Vernodalidimers A and B, novel orthoester elemanolide dimers from seeds of Vernonia anthelmintica

Two novel elemanolide dimers, vernodalidimers A (1) and B (2), possessing a rare tricyclic ortho ester moiety, were isolated from the seeds of Vernonia anthelmintica. Their structures were elucidated by 1D and 2D NMR data and CD spectra. Vernodalidimers A (1) and B (2) exhibited potent cell growth inhibitory activity against HL-60 cells (IC₅₀ 0.72 and 0.47 μM, respectively).     

Novel Designs for Centrifugal Countercurrent chromatography: V. Comparative Studies on Performance of Various Column Configurations

The conventional toroidal coil in centrifugal countercurrent chromatography has a low level of stationary phase retention, since a half of each helical turn is entirely occupied by the mobile phase. In order to cope with this problem, several new column designs including zigzag, saw-tooth and figure-8 patterns have been introduced and their performance was compared in terms of retention of the stationary phase (Sf), peak resolution (Rs), theoretical plate number (N) and column pressures. Overall results of experiments indicate that the figure-8 column yields the highest Rs when the lower phase is used as the mobile phase. Since the column pressure of all these new columns are much lower than that in the traditional toroidal coil column, the separation efficiency can be improved using a long separation column without a risk of column damage by high back pressure.