Development of coumarin-inspired bifunctional hybrids as a new class of anti-Alzheimer's agents with potent efficacy.

Considering the multifactorial and complex nature of Alzheimer's disease and the requirement of an optimum multifunctional anti-Alzheimer's agent, a series of triazole tethered coumarin-eugenol hybrid molecules was designed as potential multifunctional anti-Alzheimer's agents using donepezil and a template. The designed hybrid molecules were synthesized a click chemistry approach and preliminarily screened for cholinesterase and Aβ aggregation inhibition. Among them, AS15 emerged as a selective inhibitor of AChE (IC = 0.

Design, synthesis and mechanistic insights into triclosan derived dimers as potential anti-plasmodials.

In pursuit of novel anti-plasmodial agents, a library of triclosan-based dimers both with and without a 1-1,2,3 triazole core were designed and synthesized in order to achieve a multitargeted approach. assessment against chloroquine-susceptible (3D7) and resistant (W2) strains identified that two of the synthesized dimers containing triazole were the most potent in the series. The most potent of the synthesized compounds exhibited IC values of 9.

Oxochlorin frameworks confining a β-hydroxyketone moiety.

Nominally, -hydroxyoxochlorins, like known 5-hydroxy-7-oxo-octaethylchlorin (9), its nickel complex [5-hydroxy-7-oxo-octaethylchlorinato]nickel(II) (9Ni), or the novel 5-hydroxy-7,17-dioxo-octaethylbacteriochlorin (10), incorporate an acetylacetonate (acac)-moiety in the enol form in their chromophore structures. X-Ray diffraction studies of the compounds show the presence of a strong H-bond between the enol and flanking β-ketone. Like acac, the functionality can be deprotonated.

Molecular Players at the Sorting Stations of Malaria Parasite .

The apicomplexan pathogenic parasite ' (Pf) is responsible for most of the malaria related mortality. It resides in and refurbishes the infected red blood cells (iRBCs) for its own survival and to suffice its metabolic needs. Remodeling of host erythrocytes involves alteration of physical and biochemical properties of the membrane and genesis of new parasite induced structures within the iRBCs.

Landfill bacteriology: Role in waste bioprocessing elevated landfill gaseselimination and heat management.

This study delves into the critical role of microbial ecosystems in landfills, which are pivotal for handling municipal solid waste (MSW). Within these landfills, a complex interplay of several microorganisms (aerobic/anaerobic bacteria, archaea or methanotrophs), drives the conversion of complex substrates into simplified compounds and complete mineralization into the water, inorganic salts, and gases, including biofuel methane gas. These landfills have dominant biotic and abiotic environments where various bacterial, archaeal, and fungal groups evolve and interact to decompose substrate by enabling hydrolytic, fermentative, and methanogenic processes.

The development of thymol-isatin hybrids as broad-spectrum antibacterial agents with potent anti-MRSA activity.

Bacterial resistance toward available therapeutic agents has become a nightmare for the healthcare system, causing significant mortality as well as prolonged hospitalization, thereby needing the urgent attention of research groups working on antimicrobial drug development worldwide. Molecular hybridization is a well-established tool for developing multifunctional compounds to tackle drug resistance. Inspired by the antibacterial profiles of isatin and thymol, along with the efficiency of a triazole linker in molecular hybridization, herein, we report the design, synthesis and antibacterial activity of a novel series of triazole tethered thymol-isatin hybrids.

Scaffold hopping based designing of selective ALDH1A1 inhibitors to overcome cyclophosphamide resistance: synthesis and biological evaluation.

Aldehyde dehydrogenase 1A1 (ALDH1A1) is an isoenzyme that catalyzes the conversion of aldehydes to acids. However, the overexpression of ALDH1A1 in a variety of malignancies is the major cause of resistance to an anti-cancer drug, cyclophosphamide (CP). CP is a prodrug that is initially converted into 4-hydroxycyclophosphamide and its tautomer aldophosphamide, in the liver.

Past, present and future of xanthine oxidase inhibitors: design strategies, structural and pharmacological insights, patents and clinical trials.

Xanthine oxidase, a molybdo-flavoenzyme, and an isoform of xanthine dehydrogenase both exist as xanthine oxidoreductase and are responsible for purine catabolism. Xanthine oxidase is more involved in pathological conditions when extensively modulated. Elevation of xanthine oxidase is not only the prime cause of gout but is also responsible for various hyperuricemia associated pathological conditions like diabetes, chronic wounds, cardiovascular disorders, Alzheimer's disease, Currently available xanthine oxidase inhibitors in clinical practice (allopurinol, febuxostat and topiroxostat) suffer from fatal side effects that pose a serious problem to the healthcare system, raising global emergency to develop novel, potent and safer xanthine oxidase inhibitors.

Physiological and behavioral assessment of Metaphire posthuma in response to clothianidin insecticide: Insights from molecular and biochemical analysis.

In the present study, Clothianidin [(E) - 1-(2 - chloro-1,3 - thiazol - 5-ylmethyl) - 3-methyl - 2- nitroguanidine] (CLO) was selected as a soil pollutant and earthworm was employed as a test organism. The various responses like biochemical and detoxification process of earthworm Metaphire posthuma towards Clothianidin at lethal and sublethal doses were studied using OECD-standardized toxicological guidelines. The present study examined the toxicity of CLO to earthworms after 28 days of exposure at conc.

Stereo/regio-selective access to substituted 3-hydroxy-oxindoles with anti-proliferative assessment and validation.

The manuscript focuses on a highly stereo-/regioselective approach for synthesizing a diverse array of substituted-3-hydroxy-2-oxindoles. The synthesized compounds were subsequently subjected to anti-proliferative assessment against various cell lines, including colorectal carcinoma, ovarian cancer, and human metastatic melanoma cancer. The structural characterization of the synthesized scaffolds was unambiguously confirmed using X-ray diffraction analysis.

Organelle-targeting ratiometric fluorescent probes: design principles, detection mechanisms, bio-applications, and challenges.

Biological species, including reactive oxygen species (ROS), reactive sulfur species (RSS), reactive nitrogen species (RNS), F, Pd, Cu, Hg, and others, are crucial for the healthy functioning of cells in living organisms. However, their aberrant concentration can result in various serious diseases. Therefore, it is essential to monitor biological species in cellular organelles such as the cell membrane, mitochondria, lysosome, endoplasmic reticulum, Golgi apparatus, and nucleus.

Synthesis, molecular docking, and biological evaluation of [3,2-]indole fused 18β-glycyrrhetinic acid derivatives against skin melanoma.

Melanoma, the most serious yet uncommon type of cancer, originates in melanocytes. Risk factors include UV radiation, genetic factors, tanning lamps and beds. Here, we described the synthesis and selective anti melanoma activity of [3,2-]indole fused 18β-glycyrrhetinic acid, a derivative of 18β-glycyrrhetinic acid in murine B16F10 and A375 human melanoma cell lines.

A folded π-system with supramolecularly oriented dipoles: single-component piezoelectric relaxor with NLO activity.

Organic molecules with an active dipole moment have a natural propensity to align in an antiparallel fashion in the solid state, resulting in zero macroscopic polarization. This primary limitation makes the material unresponsive to switching with electric fields, mechanical forces, and to intense laser light. A single-component organic material that bestows macroscopic dipole-driven electro-mechanical and optical functions, , piezoelectric, ferroelectric and nonlinear optical (NLO) activity, is unprecedented due to the design challenges imparted by crystal symmetry and dipole orientations.

Metsulfuron-methyl induced physiological, behavioural and biochemical changes in exotic (Eisenia fetida) and indigenous (Metaphire posthuma) earthworm species: Toxicity and molecular docking studies.

In modern agricultural practices, Metsulfuron-methyl (sulfonylurea herbicide) is widely employed to inhibit the weeds and grasses. The current study revealed that Metaphire posthuma was more sensitive than Eisenia fetida against Metsulfuron-methyl (MSM). The LC values for Eisenia fetida were 2884.

Room-temperature highly sensitive and selective NHgas sensor using vertically aligned WSnanosheets.

Here, we report the room temperature (35 °C) NHgas sensor device made from WSnanosheets obtained via a facile and low-cost probe sonication method. The gas-sensing properties of devices made from these nanosheets were examined for various analytes such as ammonia, ethanol, methanol, formaldehyde, acetone, chloroform, and benzene. The fabricated gas sensor is selective towards NHand exhibits excellent sensitivity, faster response, and recovery time in comparison to previously reported values.

The genotoxic, cytotoxic and growth regulatory effects of plant secondary metabolite β-caryophyllene on polyphagous pest Spodoptera litura (Fabricius) (Lepidoptera: Noctuidae).

Use of secondary metabolites as an alternative to organic pesticides is an eco-friendly and safe strategy in pest management. β-caryophyllene [(1R,4E,9S)-4,11,11-trimethyl-8-methylene bicyclo [7.2.

Humidity-Tolerant Room-Temperature Selective Dual Sensing and Discrimination of NH and NO Using a WS/MWCNT Composite.

Continuous detection of toxic and hazardous gases like nitric oxide (NO) and ammonia (NH) is needed for environmental management and noninvasive diagnosis of various diseases. However, to the best of our knowledge, dual detection of these two gases has not been previously reported. To address the challenge, we demonstrate the design and fabrication of low-cost NH and NO dual gas sensors using tungsten disulfide/multiwall carbon nanotube (WS/MWCNT) nanocomposites as sensing channels which maintained their performance in a humid environment.

DOE-based synthesis of gellan gum-acrylic acid-based biodegradable hydrogels: screening of significant process variables and field studies.

The current study uses the free radical graft copolymerization of acrylic acid as a monomer, ,-methylene-bis-(acrylamide) as a crosslinker and ammonium persulfate as an initiator to synthesise GG-cl-poly(AA) hydrogels based on gellan gum utilising response surface methodology (RSM). A full factorial design was used to obtain the greatest percent swelling ( ), and key process variables were determined using the Pareto chart. To make the procedure cost-effective, a multiple regression model employing ANOVA projected a linear model with a maximum percentage swelling of 556 at the lowest concentration of all three studied factors.

The role of particulate matter in reduced visibility and anionic composition of winter fog: a case study for Amritsar city.

Severe fog events during winter months in India are a serious concern due to the higher incidence of road accidents, flight delays and increased occurrence of respiratory diseases. The present paper is an attempt to study the twenty fog samples collected from the rooftop of an academic building of Guru Nanak Dev University, Amritsar, India from November 2017 to January 2018. Fog samples were analysed for various parameters pH, electrical conductivity (EC), chloride (Cl), nitrate (NO ) and sulphate (SO ) levels.

Coronene diimide-based 'bowl' nanostructures as red emitters for the analysis of latent fingerprints and metal ion detection.

We report an NIR-based photoluminescent material, namely benzo-coronene diimide (CDI 2), and its use in the visualization of latent fingerprints (LFPs) and in the metal ion detection in an aqueous medium. CDI 2 exhibited nano-sized interlinked fibre structures forming 'bowl' shaped nanoarchitectures as red emitters with the Commission Internationale de l'Eclairage (CIE) coordinates (, ) of (0.67, 0.

Arenesulfonyl indole: new precursor for diversification of C-3 functionalized indoles.

Arenesulfonyl indoles, bearing a good leaving group, are effective precursors for vinylogous imine intermediates which are generated under basic conditions. This intermediate can readily react with other nucleophilic reagents to obtain C-3 substituted indole derivatives. In the last few years, a plethora of exciting synthetic applications of this substrate have been exploited.

high pressure neutron diffraction and Raman spectroscopy of 20BaO-80TeO glass.

The short-range structure of 20BaO-80TeO glass was studied by high pressure neutron diffraction and high pressure Raman spectroscopy. Neutron diffraction measurements were performed at the PEARL instrument of the ISIS spallation neutron source up to a maximum pressure of 9.0 ± 0.

Development of mitochondrial replacement therapy: A review.

Mitochondrial replacement therapy (MRT) is a new form of reproductive invitro fertilization (IVF) which works on the principle of replacing a women's abnormal mitochondrial DNA (mt-DNA) with the donor's healthy one. MRT include different techniques like spindles transfer (ST), pronuclear transfer (PNT) or polar body transfer (PBT). Transmission of defective mitochondrial DNA to the next generation can also be prevented by using these approaches.