Effect of Donor-Acceptor Chromophores on Photophysical Properties of Newly Synthesized Pyrazolo-Pyrrolo-Pyrimidines (PPP)

Novel pyrazolo-pyrrolo-pyrimidine (PPP) derivatives having remarkable photophysical properties are designed with the help of theoretical semiempirical calculations. These compounds then synthesized successfully and studied effect of substituents on its photophysical properties.

Effect of Specific Solute-Solvent Interaction and Electron Donor-Acceptor Substituents of Novel Pyrazolo Naphthyridines on Fluorescence

Heterocyclic orthoaminoaldehyde such as 4-amino-3-(4-phenyl)-1-phenyl-1H-Pyrazolo[3,4-b]pyridine-5-carbaldehyde was synthesized by multistep reactions involving reduction of azido derivative 2 with LAH to yield aminoalcohol 3 and oxidation of it with MnO(2) to aminoaldehyde 4.The pyridine ring annulated on to 4 by Friedl?nder condensation using acetophenones in presence of base to obtained pyrazolo[3,4-h][1,6]naphthyridine 5 in excellent yield. Study of photophysical properties of 5 revealed that the absorption and emission of them depends up on the substituents present on benzene ring in newly annulated pyridine ring.     

1,2,3-Triazolyl-tetrahydropyrimidine Conjugates as Potential Sterol Carrier Protein-2 Inhibitors: Larvicidal Activity against the Malaria Vector Anopheles arabiensis and In Silico Molecular Docking Study

Alteration of insect growth regulators by the action of inhibitors is becoming an attractive strategy to combat disease-transmitting insects. In the present study, we investigated the larvicidal effect of 1,2,3-triazolyl-pyrimidinone derivatives against the larvae of the mosquito Anopheles arabiensis, a vector of malaria. All compounds demonstrated insecticidal activity against mosquito larvae in a dose-dependent fashion. A preliminary study of the structure–activity relationship indicated that the electron-withdrawing substituent in the para position of the 4-phenyl-pyrimidinone moiety enhanced the molecules’ potency. A docking study of these derivatives revealed favorable binding affinity for the sterol carrier protein-2 receptor, a protein present in the intestine of the mosquito larvae. Being effective insecticides against the malaria-transmitting Anopheles arabiensis, 1,2,3-triazole-based pyrimidinones represent a starting point to develop novel inhibitors of insect growth regulators.     

Targeting Akt/NF-κB/p53 Pathway and Apoptosis Inducing Potential of 1,2-Benzenedicarboxylic Acid,Bis (2-Methyl Propyl) Ester Isolated from Onosma bracteata Wall. against Human Osteosarcoma (MG-63) Cells

Onosma bracteata Wall. is an important medicinal and immunity-enhancing herbs. This plant is commonly used in the preparation of traditional Ayurvedic drugs to treat numerous diseases. Inspired by the medicinal properties of this plant, the present study aimed to investigate the antiproliferative potential and the primary molecular mechanisms of the apoptotic induction against human osteosarcoma (MG-63) cells. Among all the fractions isolated from O. bracteata, ethyl acetate fraction (Obea) showed good antioxidant activity in superoxide radical scavenging assay and lipid peroxidation assay with an EC₅₀ value of 95.12 and 80.67 µg/mL, respectively. Silica gel column chromatography of ethyl acetate (Obea) fraction of O. bracteata yielded a pure compound, which was characterized by NMR, FTIR, and HR-MS analysis and was identified as 1,2-benzene dicarboxylic acid, bis (2-methyl propyl) ester (BDCe fraction). BDCe fraction was evaluated for the antiproliferative potential against human osteosarcoma MG-63, human neuroblastoma IMR-32, and human lung carcinoma A549 cell lines by MTT assay and exhibited GI₅₀ values of 37.53 μM, 56.05 μM, and 47.12 μM, respectively. In MG-63 cells, the BDCe fraction increased the level of ROS and simultaneously decreased the mitochondria membrane potential (MMP) potential by arresting cells at the G₀/G₁ phase, suggesting the initiation of apoptosis. Western blotting analysis revealed the upregulation of p53, caspase3, and caspase9 while the expressions of p-NF-κB, p-Akt and Bcl-xl were decreased. RT-qPCR studies also showed upregulation in the expression of p53 and caspase3 and downregulation in the expression of CDK2, Bcl-2 and Cyclin E genes. Molecular docking analysis displayed the interaction between BDCe fraction with p53 (−151.13 kcal/mol) and CDK1 (−133.96 kcal/mol). The results of the present work suggest that the BDCe fraction has chemopreventive properties against osteosarcoma (MG-63) cells through the induction of cell cycle arrest and apoptosis via Akt/NF-κB/p53 pathways. This study contributes to the understanding of the utilization of BDCe fraction in osteosarcoma treatment.     

安全闪存——网联汽车和工业应用中安全问题的解决之道

随着汽车和工业市场中自动化和互联革命的推进,边缘节点正在迅速成为网络攻击的目标.软件更新、远程捕获诊断数据以及远程端点与基础设施之间的通信变得越来越普遍,因此容易遭受网络攻击和其它安全威胁.随着半导体技术的进步,工艺尺寸不断缩小,将闪存嵌入到包含硬件安全模块(HSM)的MCU中也变得越来越困难,因此外置闪存的需求不断增...     

Reducing Environmental Plastic Pollution by Designing Polymer Materials for Managed End-of-Life

Plastics are widely used synthetic materials in various industries worldwide. The abundance of plastics, which are mainly carbon-based polymers, has led to a significant accumulation of plastic waste in landfills and the environment due to their durability and affordability. Although plastic pollution of the oceans has been known for many years, there is still limited knowledge about the composition, distribution, impact, and fate of plastic waste in the environment. In this review, the focus is on environmental pollution by plastics, highlighting the source (feedstock) and degradation behavior of these materials. The goal is to provide insights for material design strategies that address the management of plastic waste at the end of its life cycle. The authors argue that the development of materials labeled marine biodegradable or universally biodegradable is not a sufficient solution on its own to address plastic pollution. Instead, it is critical to incorporate practical plans for recovery and treatment into material and product design principles. These plans should be based on existing systems or possibly developed in parallel. In summary, this article highlights the widespread pollution of the environment by plastics and emphasizes the need for comprehensive material design strategies that include not only biodegradability but also practical recovery and treatment methods. By considering the entire lifecycle of plastics, we can work to reduce the harmful impact of plastic waste on our planet.     

3D highly porous microspherical morphology of NiO nanoparticles for supercapacitor application

Journal of Solid State Electrochemistry - In the present work, the effect of reaction temperature and urea concentration on the electrochemical performance of NiO nanoparticles is investigated. The...     

Total Synthesis of (E/Z) des-Hydroxy Triticone A and B

The first total synthesis of des-hydroxy triticone A and B was achieved in 12 steps. The highly chemoselective, base mediated iodolactamization of olefins with N-OMe amide motif is a key highlight of the synthesis.     

Analytical method development and validation for the simultaneous estimation of quercetin,berberine, rutin and curcumin in a polyherbal formulation using high-performance thin-layer chromatography

JPC – Journal of Planar Chromatography – Modern TLC - People all over the world are affected by the chronic, disabling autoimmune illness known as rheumatoid arthritis (RA). Herbal...     

Fuzzy-based techniques for clustering in wireless sensor networks (WSNs): Recent advances,challenges, and future directions

A wireless sensor network (WSN) is a network of tiny sensors deployed to collect data. These sensors are powered with batteries that have limited power. Recharging and/or replacement of these batteries, however, are not always feasible. Over the past few years, WSN applications are being deployed in diverse fields such as military, manufacturing, healthcare, agriculture, and so on. With the ever-increasing applications of WSNs, improving the energy efficiency of the WSNs still remains to be a challenge. Applying fuzzy logic to the problem of clustering exploits the uncertainty associated with the factors that affect the lifetime of these sensors and enables the development of models that would improve their performance in real-world applications. We present a comprehensive review of various fuzzy-based techniques for clustering in WSNs whose main goal is to optimize energy usage in WSNs while simultaneously improving their overall performance.