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Novel azo dyes containing a hydrazide-hydrazone moiety linked to the benzothiazole nucleus are synthesized effectively in this study. The primary purpose of the study was to identify the best dyeing parameters, such as shade, temperature, pH, and time, in order to better understand the behaviour of dispersed dyes during polyester dyeing. To achieve excellent colour strength in value (K/S = 26), the ideal dyeing conditions for disperse dye 4 were 30 min, pH of 8, and 110 °C at shade 3%. While the ideal dyeing conditions for disperse dyes dye 10 and dye 11 were 30 min, pH of 2, and 130 °C at a shade of 3%. Depending on the coupler moieties, the coloured polyester samples ranged in hue from beige to dark brown. Furthermore, the impact of substituent’s was examined in relation to colour strength (K/S) measures and colourimetric coordinates (CIEL*a*b*) of dyed polyester fabrics. The synthesized dispersed dyes are good options for giving polyester textiles a variety of stable hues and very good colour strength as well as exceptional fastness to light, washing, and crocking.

In this study, a novel series of 1,2,4-triazolo[4,3- a ]quinoxalines containing a sulfonamide moiety was designed and synthesized through regioselective synthesis from 2 and/ 3-hydrazino-6-(pyrrolidin-1-ylsulfonyl)quinoxaline derivatives 5 and 7 . The structures of two isomers were confirmed and characterized by IR, 1 H NMR, 13 C NMR, and elemental analysis data. The synthesized 1,2,4-triazolo[4,3- a ]quinoxaline derivatives 8–13 were evaluated for their antidiabetic activities by targeting α-amylase and α-glucosidase, as well as for their anti-Alzheimer activity by targeting acetylcholinesterase (AChE) at a concentration of 100 µM. Structure-activity relationship (SAR) analysis was conducted for all analogs, emphasizing the nature of the substituent groups at position one of the triazole nucleus and the positioning of the sulfonamide moiety. For α-amylase and α-glucosidase activity, the designed compounds exhibited moderate to good activity, with inhibitory percentage values ranging from 21.85 ± 0.01% to 64.70 ± 0.02% and from 23.93 ± 0.01% to 75.36 ± 0.01%, respectively. The N -allyl-[1,2,4]triazolo[4,3- a ]quinoxalin-1-amine derivative 10a demonstrated the most significant inhibitory activity, with percentages of 64.70 ± 0.02% and 75.36 ± 0.01% against α-amylase and α-glucosidase, respectively, in comparison to acarbose (IP = 67.33 ± 0.01% and 57.79 ± 0.01%). Furthermore, the 1,2,4-triazolo[4,3- a ]quinoxaline derivatives 8–13 exhibited low to moderate inhibitory percentages against the acetylcholinesterase enzyme, except for the 1-methyl-[1,2,4]triazolo[4,3- a ]quinoxaline derivative 11b which demonstrated the highest inhibitory percentage of 44.78 ± 0.01%, compared to donepezil (IP = 67.27 ± 0.60%). Moreover, the promising derivative 10a demonstrated exceptional inhibitory activity, exhibiting IC 50 values of 3.46 ± 0.06 µM and 6.89 ± 0.09 µM against α-glucosidase and α-amylase, respectively, when compared to acarbose, which has IC 50 values of 4.27 ± 0.06 µM and 5.90 ± 0.09 µM. Finally, molecular docking simulations were performed for compound 10a within α-amylase (PDB: 2QV4) and α-glucosidase (PDB: 3W37), while compound 11b was analyzed within acetylcholinesterase (AChE) (PDB: 4EY7) to assess binding affinity and to explore the binding interactions with the active sites of the enzymes.

The main objective of research worldwide is targeting particular genes and proteins vital for the development and viability of cancer cells. This recent research explores the synthesis and biological evaluation of N -tosyl indole-3-carbaldehyde based hydrazones 5(a-r) as anti-breast cancer (BC) agents. Two cell lines were employed to evaluate newly synthesized compounds in-vitro; the normal epithelial breast cell line MCF-10 A and the MDA-MB-231 BC cell line. All the synthesized compounds demonstrated significant activity against the BC cell line MDA-MB-231. Compound 5p ( IC 50  = 12.2 ± 0.4 µM) with a naphthyl group, exhibited promising potential against triple-negative breast cancer (TNBC) cell line MDA-MB-231. The structures of the compounds 5(a-r) were confirmed by using different characterization techniques such as FT-IR, ¹H NMR, ¹³C NMR, and QTOF HRMS. Molecular docking study demonstrates that compound 5q binds strongly to EGFR (T790M/L858R mutant) with binding energy − 11.533 kcal/mol. However, molecular dynamics show stable interactions with protein 3W2S over 100 ns, supported by favorable RMSD, RMSF and SASA values. These findings hypothesize that compound 5q exerts its anticancer effect through stable molecular interactions. All synthesized compounds significantly reduced viability in MDA-MB-231 cells compared to normal MCF-10 A cells ( p  < 0.0001), indicating selective cytotoxicity toward breast cancer cells.

A new series of 6-hydroxychromone-based thiosemicarbazones 4(a-p) was synthesized and assessed for their antidiabetic (α-Glucosidase and α-Amylase inhibition) as well as antioxidant (2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2´-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS)) activities. Among the synthesized compounds, compound 4k (IC 50  = 1.18 ± 0.19 µg/mL) emerged as the promising α-Glucosidase inhibitor, significantly outperforming the reference drug Acarbose (IC 50  = 7.33 ± 0.13 µg/mL). For α-Amylase inhibition, compound 4 g (IC 50  = 13.61 ± 2.04 µg/mL) demonstrated excellent activity, compared to Acarbose (IC 50  = 43.15 ± 5.22 µg/mL). In antioxidant assays, compound 4o (IC 50  = 15.30 ± 1.70 µg/mL) exhibited the strongest DPPH radical scavenging effect, and compound 4 g (IC 50  = 6.06 ± 0.15 µg/mL) showed the highest ABTS scavenging activity, surpassing the standard antioxidant Trolox (IC 50  = 30.20 ± 5.14 & 18.19 ± 2.47 µg/mL, respectively). Remarkably, these derivatives showed greater efficacy compared to standard inhibitors, underscoring their promise as novel candidates for antidiabetic and antioxidant drug development. Molecular docking analysis demonstrated strong binding and critical interactions within the enzyme active sites. MD simulations confirmed the stability of 4k-α-Glucosidase and 4 g-α-Amylase, with RMSD values below 3.6 Å, low RMSF (< 2.8 Å) at the binding site, and sustained key interactions with Phe 158 and Tyr 151 , respectively. The network pharmacology further supported the findings of molecular docking and simulation analysis.

The most prevalent degenerative brain disease, Alzheimer’s disease (AD), is characterized by cognitive function impairment. The ability to code new memories is lost in AD patients, and their lives are very challenging. Inhibitors of cholinesterase (ChE) and monoamine oxidase (MAO) have drawn interest as potential therapies for AD. To combat Alzheimer’s disease (AD), a new class of Coumarin-hydrazone hybrids has been synthesized 3(a-m). Compounds 3a , 3e , and 3l exhibited significant acetylcholinesterase (AChE) inhibitory activity with low IC 50 values of 7.40 ± 0.14 µM, 8.01 ± 0.70 µM, and 8.54 ± 1.01 µM, respectively. Additionally, these compounds, along with 3k , demonstrated potent butyrylcholinesterase (BChE) inhibition, with IC 50 values from 65.41 ± 4.55 µM to 74.98 ± 5.30 µM, highlighting their dual cholinesterase inhibitory potential. Compound like 3a (1.44 ± 0.03 µM), 3e (1.51 ± 0.13 µM), and 3l (1.65 ± 0.03 µM) display robust MAO-A inhibition, suggesting high potency. To see how the most potent inhibitor chemicals affected the substrate–enzyme relationship, enzyme kinetic tests were conducted in addition to enzyme inhibition investigations. Compound 3e may function as a dual binding site AChE inhibitor, according to docking studies in addition to in vitro testing.

Local measurement of deformations of a soil specimen has become inevitable for accurate determination of soil stiffness in triaxial tests. Although there are now many devices that can be used to perform this task, each has its own advantages and limitations that render development of new devices with better desirable features. This paper presents an innovative device called spring deformation gauge (SDG) that has many advantages over many of the existing devices and can be readily manufactured in both research and commercial laboratories. The device is based on using a highly flexible, yet very strong metal strip of spring steel secured between two stiff, stainless steel L-shaped legs; the spring strip is provided with four strain gauges. With this arrangement, local deformation of a specimen is transferred into significant bending in the metal strip and elongation or shortening of the strain gauges. In addition to being very cost effective, the SDG is characterized by the ability to control both range and resolution of measured deformation, its linear output, and a clever pinning mechanism that protects it from being damaged when it goes out of range. Success of the SDG was demonstrated in a true K0 test on carbonate sand.

Cadmium (Cd) is an environmental pollutant known as endocrine disruptor . Cd has been reported to induce perturbations of the testicular functions and the subsequent decline of the male fertility of both animals and humans. Chlorella vulgaris (ChV) a species of green microalga has been reported to have multiple beneficial activities such as anti-inflammatory, antioxidant, and antiapoptotic effects. Thus, this work was conducted to declare the benefits of Chlorella vulgaris (ChV) (500 mg/kg doses) against cadmium chloride CdCl2 (2 mg/kg doses) toxicity on the main and accessory reproductive organs’ weight, structure, and function of male rats. Briefly, 40 adult male rats in 4 groups (n = 10) were used as follows; control, ChV, CdCl2, and CdCl2+ChV. (i) The 1st group was kept as control fed on pellet chow and water ad libitum. (ii) The second group is Chlorella vulgaris (ChV) group fed with C. vulgaris alga for 10 days (500 mg/kg BW). (iii) The third group was administrated CdCl2 (2mg/kg BW) via subcutaneous injection (S/C) daily for 10 days. (iv) The fourth group administered both CdCl2 and ChV with the abovementioned doses daily for successive 10 days. Our observations declared that cadmium exhibited an adverse influence on the testes and prostate gland architecture indicated by seminiferous tubule destruction, testicular edema, degeneration of Leydig cells, and prostate acini damage. All together affect the epididymal semen quality and quantity including sperm viability, motility, and count. Interestingly, ChV could restore the testicular architecture and spermatozoa regeneration accompanied by semen quality improvement and increased reproductive hormones including testosterone. On the other side, ChV suppresses reactive oxygen species (ROS) formation via enhancement the antioxidant-related genes in the testicular tissue including SOD, CAT, GSH, and MDA and maintaining spermatocyte survival via suppression of apoptotic related genes including caspase3 and activating steroidogenic related genes including StAR and HSD17β3 in the cadmium-treated testes. In this study, ChV could enhance male fertility under normal or stressful conditions and ameliorate the adverse effects of hazardous heavy metals that are widely distributed in our environment.

Introduction Cervicogenic headache (CGH) is a serious condition manifested by upper cervical facet joints dysfunction. Mulligan upper cervical sustained natural apophyseal glide was noted to be effective in CGH but Mulligan upper cervical manual traction (MUCMT) has not yet been investigated. The purpose of the study was to compare the effect of MUCMT vs. traditional treatment (TT) in patients with CGH. Methods A randomized controlled prospective parallel single-blind trial was performed. Overall, 30 patients with CGH aged 30–55 years were randomly and equally allocated into the MUCMT group (A) and TT group (B) by using permuted block randomization. Group A participants were treated by TT and MUCMT while group B received hot packs, transcutaneous electrical nerve stimulation, and deep cervical flexors strengthening exercise. Patients gained 3 sessions every week for 3 weeks followed by home exercise for 3 months. Pre-treatment, post-treatment, and follow-up values for all outcome measures were recorded. The primary outcome was headache intensity. Secondary outcomes involved headache frequency, headache duration, neck disability index, and upper cervical rotation range of motion. Results Within groups, statistical analysis revealed a significant difference in the comparison of pre- vs. post-treatment and post-treatment vs. follow-up mean values of all outcomes. Between groups, no statistical significance was observed in post-treatment and follow-up data, with 1 exception regarding upper cervical range of motion in favour of MUCMT. Conclusions MUCMT is an effective treatment in patients with CGH, mainly with regard to upper cervical rotation range of motion.

Unlike clays, sands may exist in a virgin condition, but at different initial void ratios. Therefore, there is no consensus in the literature as to the definition of the normal compression line for sands. On the basis of experimental evidence, this paper presents a new simple normalisation scheme to unify the compression response of sands. The normalisation scheme incorporates both the initial void ratio and its corresponding equivalent stress on the limiting compression line as normalising parameters. The novelty of the new normalisation scheme is that it is not only consistent with the framework of critical state soil mechanics, but it is also conceptually in line with recent studies on crushability of soils. The validity of the new normalisation scheme is verified against a wide range of experimental data from isotropic and 1-D compression tests on both sands and clays. It is also shown that a unified compression relationship can be obtained for both clays and sands by taking into account the differences in the compression index at high pressure. Similarities between the compression curves and the critical state line for different soils are also examined, and it is shown that the critical state line for clays and sands can be uniquely represented using the proposed normalisation scheme. Areas for further research, where the new normalisation scheme is deemed valuable, are highlighted.

In this study, a novel series of 1,2,4-triazolo[4,3-a]quinoxalines containing a sulfonamide moiety was designed and synthesized through regioselective synthesis from 2 and/ 3-hydrazino-6-(pyrrolidin-1-ylsulfonyl)quinoxaline derivatives 5 and 7. The structures of two isomers were confirmed and characterized by IR,1H NMR,13C NMR, and elemental analysis data. The synthesized 1,2,4-triazolo[4,3-a]quinoxaline derivatives 8-13 were evaluated for their antidiabetic activities by targeting α-amylase and α-glucosidase, as well as for their anti-Alzheimer activity by targeting acetylcholinesterase (AChE) at a concentration of 100 µM. Structure-activity relationship (SAR) analysis was conducted for all analogs, emphasizing the nature of the substituent groups at position one of the triazole nucleus and the positioning of the sulfonamide moiety. For α-amylase and α-glucosidase activity, the designed compounds exhibited moderate to good activity, with inhibitory percentage values ranging from 21.85 ± 0.01% to 64.70 ± 0.02% and from 23.93 ± 0.01% to 75.36 ± 0.01%, respectively. The N-allyl-[1,2,4]triazolo[4,3-a]quinoxalin-1-amine derivative 10a demonstrated the most significant inhibitory activity, with percentages of 64.70 ± 0.02% and 75.36 ± 0.01% against α-amylase and α-glucosidase, respectively, in comparison to acarbose (IP = 67.33 ± 0.01% and 57.79 ± 0.01%). Furthermore, the 1,2,4-triazolo[4,3-a]quinoxaline derivatives 8-13 exhibited low to moderate inhibitory percentages against the acetylcholinesterase enzyme, except for the 1-methyl-[1,2,4]triazolo[4,3-a]quinoxaline derivative 11b which demonstrated the highest inhibitory percentage of 44.78 ± 0.01%, compared to donepezil (IP = 67.27 ± 0.60%). Moreover, the promising derivative 10a demonstrated exceptional inhibitory activity, exhibiting IC50 values of 3.46 ± 0.06 µM and 6.89 ± 0.09 µM against α-glucosidase and α-amylase, respectively, when compared to acarbose, which has IC50 values of 4.27 ± 0.06 µM and 5.90 ± 0.09 µM. Finally, molecular docking simulations were performed for compound 10a within α-amylase (PDB: 2QV4) and α-glucosidase (PDB: 3W37), while compound 11b was analyzed within acetylcholinesterase (AChE) (PDB: 4EY7) to assess binding affinity and to explore the binding interactions with the active sites of the enzymes.In this study, a novel series of 1,2,4-triazolo[4,3-a]quinoxalines containing a sulfonamide moiety was designed and synthesized through regioselective synthesis from 2 and/ 3-hydrazino-6-(pyrrolidin-1-ylsulfonyl)quinoxaline derivatives 5 and 7. The structures of two isomers were confirmed and characterized by IR,1H NMR,13C NMR, and elemental analysis data. The synthesized 1,2,4-triazolo[4,3-a]quinoxaline derivatives 8-13 were evaluated for their antidiabetic activities by targeting α-amylase and α-glucosidase, as well as for their anti-Alzheimer activity by targeting acetylcholinesterase (AChE) at a concentration of 100 µM. Structure-activity relationship (SAR) analysis was conducted for all analogs, emphasizing the nature of the substituent groups at position one of the triazole nucleus and the positioning of the sulfonamide moiety. For α-amylase and α-glucosidase activity, the designed compounds exhibited moderate to good activity, with inhibitory percentage values ranging from 21.85 ± 0.01% to 64.70 ± 0.02% and from 23.93 ± 0.01% to 75.36 ± 0.01%, respectively. The N-allyl-[1,2,4]triazolo[4,3-a]quinoxalin-1-amine derivative 10a demonstrated the most significant inhibitory activity, with percentages of 64.70 ± 0.02% and 75.36 ± 0.01% against α-amylase and α-glucosidase, respectively, in comparison to acarbose (IP = 67.33 ± 0.01% and 57.79 ± 0.01%). Furthermore, the 1,2,4-triazolo[4,3-a]quinoxaline derivatives 8-13 exhibited low to moderate inhibitory percentages against the acetylcholinesterase enzyme, except for the 1-methyl-[1,2,4]triazolo[4,3-a]quinoxaline derivative 11b which demonstrated the highest inhibitory percentage of 44.78 ± 0.01%, compared to donepezil (IP = 67.27 ± 0.60%). Moreover, the promising derivative 10a demonstrated exceptional inhibitory activity, exhibiting IC50 values of 3.46 ± 0.06 µM and 6.89 ± 0.09 µM against α-glucosidase and α-amylase, respectively, when compared to acarbose, which has IC50 values of 4.27 ± 0.06 µM and 5.90 ± 0.09 µM. Finally, molecular docking simulations were performed for compound 10a within α-amylase (PDB: 2QV4) and α-glucosidase (PDB: 3W37), while compound 11b was analyzed within acetylcholinesterase (AChE) (PDB: 4EY7) to assess binding affinity and to explore the binding interactions with the active sites of the enzymes.