Design of Experiment Approach for the Development and Validation of a Stability-Indicating High-Performance Thin-Layer Chromatography Method for the Estimation of Metformin Hydrochloride and Ursodeoxycholic Acid in Pharmaceutical Dosage Form

JPC – Journal of Planar Chromatography – Modern TLC - In the present study, a design of experiment (DoE) approach was used to optimize chromatographic conditions for the development of...     

Development of a Surfactant/Platinum Composite for Sensitive Cardio‐selective Beta Blocker Detection and their Theoretical Studies

An electrooxidative behavior of beta‐blocker drug esmolol was thoroughly investigated by using glassy carbon electrode modified with sodium dodecyl sulfate‐based platinum nanoparticles. The designed nanosensor exhibited remarkable electro‐catalytic effect by dramatically boosting the signal of the esmolol as compared to the bare electrode with detection limit up to picomolar. The effects of pH, scan rate, temperature, deposition potential, deposition time, effect of electrolyte and interfering agents were investigated to optimize conditions for getting intense signal of the analyte. Under optimized experimental conditions, a linear calibration plot for esmolol with a detection limit of 60 pM was obtained. The analyte sensing ability of the modified electrode was supported by the application of theoretical studies that showed favorable interaction between sodium dodecyl sulfate/platinum nanoparticles composite and esmolol. In this study, our aim was to developed a nanosensor for the sensitive detection of esmolol by electrochemical assay. We tried a lot of different modification style and modifiers for creating a sensitive nanosensor for esmolol. This nanosensor can be applied to the esmolol in serum sample without using any further separation, evaporation or precipitation steps. Application could apply in serum sample to test accuracy of our sensor and method. The high recovery results were observed in serum study.     

A new sulphated flavone and other phytoconstituents from the leaves of Tetracera indica Merr. and their alpha-glucosidase inhibitory activity

The bioactivity guided fractionation of Tetracera indica leaves crude ethanolic extract has afforded the isolation and characterization of six compounds including a new natural product viz., 5,7-dihydroxyflavone-O-8-sulphate (1) and five known flavonoids (2–6). The structures of the compounds were elucidated using 1D and 2D NMR and HRESIMS spectroscopic analyses. All the isolated compounds were evaluated for their in vitro inhibitory activity against alpha-glucosidase. Compound 1, 5 and 6 showed strong alpha-glucosidase inhibitory activity, 3 and 4 displayed weak activity while compound 2 was inactive. The interactions of the active compounds with alpha-glucosidase were further investigated using molecular docking to confirm their antidiabetic potential.     

Synthetic Approaches to Star‐Shaped Molecules with 1,3,5‐Trisubstituted Aromatic Cores

Herein, we summarize the synthetic approaches that have been developed for the synthesis of star‐shaped molecules. Typically, to design such highly functionalized molecules, simple building blocks are first assembled through trimerization reactions, starting from commercially available starting materials. Then, these building blocks are synthetically manipulated to generate extended star‐shaped molecules. We also discuss the syntheses of star‐shaped molecules that contain 2,4,6‐trisubstituted 1,3,5‐triazine or 1,3,5‐trisubstituted benzene rings as a central core and diverse substituted styrene, phenyl, and fluorene derivatives at their periphery, which endows these molecules with extended conjugation. A variety of metal‐catalyzed reactions, such as Suzuki, Buchwald–Hartwig, Sonogashira, Heck, and Negishi cross‐coupling reactions, as well as metathesis, have been employed to functionalize a range of star‐shaped molecules. The methods described herein will be helpful for designing a wide range of intricate compounds that are highly valuable in the fields of supramolecular chemistry and materials science. Owing to space limitations, we will not cover all of the publications on this topic. Instead, we will focus on examples that were reported by our research group and other relevant recent literature. Apart from the trimerization sequence, this Minireview has been structured based on the key reactions that were used to prepare the star‐shaped molecules and other higher analogues. Finally, some examples that do not fit into this classification are discussed.     

Exploiting Strained Rings in Chelation Guided C−H Functionalization: Integration of C−H Activation with Ring Cleavage

Strained ring systems are regarded as privileged coupling partners in directed C?H bond functionalization and have emerged as a potential research area in organic synthesis. The inherent ring strain in these systems acts as a driving force, allowing the facile construction of diversified structural scaffolds via integrating C?H activation and ring‐scission. The mechanistic underpinnings allows the implementation of a plethora of C?H bonds across plentiful organic substrates, including the less reactive alkyl ones. Considering the synthetic space, this area will foster developments of novel synthetic methods in chelation guided C?H functionalization. This review will focus on recent developments in transition‐metal catalyzed chelation assisted concomitant C?H activation and ring scission of strained rings to attain molecular complexity.     

Solar wind driven electrostatic instabilities with generalized (r,q) distribution function

Using Boltzmann–Vlasov kinetic model, a currentless ion acoustic instability driven by stream of solar wind plasma is studied in a non‐thermal distributed electrons and ions. The non‐thermal distribution considered here is the generalized distribution which has low energetic flat‐top and velocity power law tail at higher energies. The instability threshold is found to be affected and depends upon the spectral indices r and q . It is found that the growth rate increases with the decrease in the value of r and increase with q . Moreover, such kinetic instability has also been discussed for three species electron–ion–dust plasma using the generalized (r, q) distribution function. Such case is of interest when the solar wind is streaming through the cometary plasma in the presence of interstellar dust and excites electrostatic instabilities. The dispersion properties and growth rates for ion‐acoustic and dust‐acoustic mode are calculated analytically and plotted for different values of the spectral indices r and q .     

Theoretical model for the effect of dust grains on self‐filamentation of a gaussian electromagnetic beam in a fully ionized plasma

A theoretical model for the effect of dust grains on the self‐filamentation of a Gaussian electromagnetic beam propagating in a fully ionized plasma has been developed by employing the energy balance of the plasma constituents, perturbed electron and ion concentrations, and temperature. In this model, neutral atom ionization, re‐integration and accumulation of electrons and ions, photoelectric emission of electrons from the surface of dust grains, as well as elastic and charging collisions have also been considered. The effective dielectric constant in the presence of dust grains has been constructed. The effect of temporal growth of dust grains on various plasma parameters for different values of the dust density has been explored. The variation of the beam width with the normalized channel of propagation has been observed for distinct dust densities and dust charge states. It is observed that the non‐linearity induced by the effective dielectric constant in the presence of dust grains increases the self‐filamentation of the beam, thus enhancing the effective critical power with the dust density. Some of the outcomes of our approach are in line with experimental observations. These outcomes may be useful for explaining space and laboratory plasma experiments as well as for future studies in complex plasmas.     

Visible-light-mediated Gomberg-Bachmann reaction: An efficient photocatalytic approach to 2-aminobiphenyls

An efficient, metal-free and highly selective protocol for the synthesis of 2-aminobiphenyls via visible-light-mediated arylation of anilines using aryl diazonium salts (Gomberg-Bachmann reaction) has been reported. The reaction is an example of photoredox catalysed direct C(sp²)–H arylation of anilines using eosin Y as an organophotoredox catalyst. The presented visible-light-mediated environmentally sustainable approach has the potential to earn a decent position among the classical and contemporary methods for the synthesis of aminobiaryls.     

Design,Synthesis, and Biological and In Silico Study of Fluorine‐Containing Quinoline Hybrid Thiosemicarbazide Analogues

A novel series of fluorine‐containing quinoline hybrid thiosemicarbazide analogues ( 8a–8l ) were synthesized and tested for their biological activities. The antibacterial results demonstrated that compounds 8d and 8l [minimal inhibitory concentration (MIC) 62.5 μg/mL] were shown to have higher biological activity than ampicillin against Escherichia coli. Compound 8b (MIC 25 μg/mL) was shown to have the highest activity than was ampicillin against Staphylococcus aureus. The antifungal results demonstrated that compound 8j (MIC 100 μg/mL) has shown good activity. Most of the targeted compounds have shown potent antimalarial activity. Compounds 8d (0.19 μg/mL), 8g (0.30 μg/mL), 8h (0.36 μg/mL), 8k (0.10 μg/mL), 8l (0.28 μg/mL), 8k (0.10 μg/mL), and 8l (0.28 μg/mL) have notable activity than does the reference drug quinine. Compounds 8d (0.27 μg/mL), 8g (0.30 μg/mL), and 8k (0.17 μg/mL) have shown excellent activity against chloroquine‐resistant strain. The MTT assay performed on peripheral blood lymphocyte cultures showed a high percentage of lymphocyte viability [ 8d (99.64), 8g (99.46), 8h (98.83), and 8k (99.51)] at a maximum dose (10 μg/mL), depicting no cytotoxicity of these compounds on human lymphocytes in vitro. A molecular docking study was performed on Pf‐DHFR‐TS inhibitor. A molecular dynamics study has shown compound 8g to have better affinity with protein. ADME‐Tox and pharmacophore study of synthesized compounds suggested prediction of active site.     

Synthesis,in vitro urease inhibitory activity and molecular docking of 3,5‐disubstituted thiadiazine‐2‐thiones

A series of 3,5‐disubstituted‐tetrahydro‐thiadiazine‐2‐thione ( 1 ‐ 16 ) have been synthesized, characterized by elemental analysis, infrared (IR), UV‐visible, ¹H NMR, ¹³C NMR, and MS spectroscopic techniques, and screened against jack bean urease. Among 16 compounds, compounds ( 1 ), ( 2 ), ( 3 ), ( 4 ), ( 6 ), ( 7 ), and ( 9 ) demonstrated excellent urease inhibitory activity with IC₅₀ values (9.8 ± 0.5, 11.0 ± 0.6, 16.0 ± 1.5, 17.2 ± 0.5, 15.4 ± 0.5, 19.7 ± 0.4, and 15.8 ± 0.2μM), respectively, even better than the standard thiourea (IC₅₀ = 21 ± 0.01μM). However, compound ( 8 ) shows an almost same level of inhibition (IC₅₀ = 22.9 ± 0.3μM), as like standard. In this work, we reported for the first time urease inhibitory activity of thiadiazine thiones and its molecular docking studies.