Synthesis, Urease Inhibition, Molecular Docking, and Optical Analysis of a Symmetrical Schiff Base and Its Selected Metal Complexes.

Designing and developing small organic molecules for use as urease inhibitors is challenging due to the need for ecosystem sustainability and the requirement to prevent health risks related to the human stomach and urinary tract. Moreover, imaging analysis is widely utilized for tracking infections in intracellular and in vivo systems, which requires drug molecules with emissive potential, specifically in the low-energy region. This study comprises the synthesis of a Schiff base ligand and its selected transition metals to evaluate their UV/fluorescence properties, inhibitory activity against urease, and molecular docking.

Synthesis, Kinetics and Computational Explorations of 4-Phenylpiperazine Bearing N-(Aryl)-3-substituted-benzamides as Auspicious Tyrosinase Inhibitors.

In the aimed research study, a new series of N-(aryl)-3-[(4-phenyl-1-piperazinyl)methyl]benzamides was synthesized, which was envisaged as tyrosinase inhibitor. The structures of these newly designed molecules were verified by IR, H-NMR, C-NMR, EI-MS and CHN analysis data. These molecules were screened against tyrosinase and their inhibitory activity explored that these 3-substituted-benzamides exhibit good to excellent potential, comparative to the standard.

Recent Development on Sensing Strategies for Small Molecules Detections.

Sensors play a critical role in the detection and monitoring of various substances present in our environment, providing us with valuable information about the world around us. Within the field of sensor development, one area that holds particular importance is the detection of small molecules. Small molecules encompass a wide range of organic or inorganic compounds with low molecular weight, typically below 900 Daltons including gases, volatile organic compounds, solvents, pesticides, drugs, biomarkers, toxins, and pollutants.

Cephalosporin as Potent Urease and Tyrosinase Inhibitor: Exploration through Enzyme Inhibition, Kinetic Mechanism, and Molecular Docking Studies.

In present study, eleven cephalosporin drugs were selected to explore their new medically important enzyme targets with inherited safety advantage. To this end, selected drugs with active ingredient, cefpodoxime proxetil, ceftazidime, cefepime, ceftriaxone sodium, cefaclor, cefotaxime sodium, cefixime trihydrate, cephalexin, cefadroxil, cephradine, and cefuroxime, were evaluated and found to have significant activity against urease (IC50 = 0.06 ± 0.

Preparation of Spice Extracts: Evaluation of Their Phytochemical, Antioxidant, Antityrosinase, and Anti--Glucosidase Properties Exploring Their Mechanism of Enzyme Inhibition with Antibrowning and Antidiabetic Studies .

Tyrosinase and -glucosidase enzymes are known as promising target candidates for inhibitors to control unwanted pigmentation and type II diabetics mellitus. Therefore, twenty extracts as enzyme inhibitors were prepared from edible spices: nutmeg, mace, star anise, fenugreek, and coriander aiming to explore their antioxidant, antibrowning, and antidiabetic potential. Results confirmed that all extracts showed potent antioxidant activity ranging from IC = 0.

Structure-based designing and synthesis of 2-phenylchromone derivatives as potent tyrosinase inhibitors: In vitro and in silico studies.

The present study describes the discovery of novel inhibitors of mushroom tyrosinase enzyme. For that purpose, a series of varyingly substituted 2-phenylchromone analogues 1-28 were synthesized and characterized in detail by various spectroscopic techniques (UV-Vis, FTIR, H NMR, C NMR) and mass spectrometry. All the derivatives (1-28) were screened in vitro for their inhibitory potential against mushroom tyrosinase enzyme.

Exploring 3-hydroxyflavone scaffolds as mushroom tyrosinase inhibitors: synthesis, X-ray crystallography, antimicrobial, fluorescence behaviour, structure-activity relationship and molecular modelling studies.

To explore new scaffolds as tyrosinase enzyme inhibitors remain an interesting goal in the drug discovery and development. In due course and our approach to synthesize bioactive compounds, a series of varyingly substituted 3-hydroxyflavone derivatives () were synthesized in one-pot reaction and screened for against mushroom tyrosinase enzyme. The structures of newly synthesized compounds were unambiguously corroborated by usual spectroscopic techniques (FTIR, UV-Vis, H-, C-NMR) and mass spectrometry (EI-MS).

Role of salicylic acid in regulating ethylene and physiological characteristics for alleviating salinity stress on germination, growth and yield of sweet pepper.

Background: During a preliminary study, effects of 0, 20, 40, and 60 mM NaCl salinity were assessed on germination rate in relation to electrolyte leakage (EL) in sweet pepper. Results explored significant rises in ethylene evolution from seeds having more EL. It was, therefore, hypothesized that excessive ethylene biosynthesis in plants due to salinity stress might be a root cause of low crop productivity.

Hydroxyl substituted benzoic acid/cinnamic acid derivatives: Tyrosinase inhibitory kinetics, anti-melanogenic activity and molecular docking studies.

The inhibition of tyrosinase is an established strategy for treating hyperpigmentation. Our previous findings demonstrated that cinnamic acid and benzoic acid scaffolds can be effective tyrosinase inhibitors with low toxicity. The hydroxyl substituted benzoic and cinnamic acid moieties of these precursors were incorporated into new chemotypes that displayed in vitro inhibitory effect against mushroom tyrosinase.

Synthesis, computational studies, tyrosinase inhibitory kinetics and antimelanogenic activity of hydroxy substituted 2-[(4-acetylphenyl)amino]-2-oxoethyl derivatives.

The over expression of melanogenic enzymes like tyrosinase caused many hyperpigmentaion disorders. The present work describes the synthesis of hydroxy substituted 2-[(4-acetylphenyl)amino]-2-oxoethyl derivatives and as antimelanogenic agents. The tyrosinase inhibitory activity of synthesized derivatives and was determined and it was found that derivative possesses excellent activity with IC = 0.

Flavonols and 4-thioflavonols as potential acetylcholinesterase and butyrylcholinesterase inhibitors: Synthesis, structure-activity relationship and molecular docking studies.

To explore new scaffolds for the treat of Alzheimer's disease appears to be an inspiring goal. In this context, a series of varyingly substituted flavonols and 4-thioflavonols have been designed and synthesized efficiently. All the newly synthesized compounds were characterized unambiguously by common spectroscopic techniques (IR, H-, C NMR) and mass spectrometry (EI-MS).

Novel Amide Derivatives as Potent Tyrosinase Inhibitors; In-vitro, In-vivo Antimelanogenic Activity and Computational Studies.

Background: Tyrosinase is involved in the melanin biosynthesis and the abnormal accumulation of melanin pigments leading to hyperpigmentation disorders. Controlling the melanogenesis could be an important strategy for treating abnormal pigmentation.

Methods: In the present study, a series of amide derivatives (3a-e and 5a-e) were synthesized aiming to inhibit tyrosinase activity and melanin production.

WMSS: A Web-Based Multitiered Surveillance System for Predicting CLABSI.

Central-line-associated bloodstream infection (CLABSI) rates are a key quality metric for comparing hospital quality and safety. Manual surveillance systems for CLABSIs are time-consuming and often limited to intensive care units (ICUs). A computer-automated method of CLABSI detection can improve the validity of surveillance.

How Does Plasma Activated Media Treatment Differ From Direct Cold Plasma Treatment?

Objective: The aim of the paper is to investigate the optimum condition for generation of Plasma Activated Media (PAM), where it can deactivate the cancer cells while minimum damage for normal cells.

Background: Over past few years, cold atmospheric Plasma-Activated Media (PAM) have shown its promising application in plasma medicine for treatment of cancer. PAM has a tremendous ability for selective anti-cancer capacity in vitro and in vivo.

Improving Prediction Accuracy of "Central Line-Associated Blood Stream Infections" Using Data Mining Models.

Prediction of nosocomial infections among patients is an important part of clinical surveillance programs to enable the related personnel to take preventive actions in advance. Designing a clinical surveillance program with capability of predicting nosocomial infections is a challenging task due to several reasons, including high dimensionality of medical data, heterogenous data representation, and special knowledge required to extract patterns for prediction. In this paper, we present details of six data mining methods implemented using cross industry standard process for data mining to predict central line-associated blood stream infections.

Influence of plasma-activated compounds on melanogenesis and tyrosinase activity.

Many organic chemists around the world synthesize medicinal compounds or extract multiple compounds from plants in order to increase the activity and quality of medicines. In this work, we synthesized new eugenol derivatives (ED) and then treated them with an N2 feeding gas atmospheric pressure plasma jet (APPJ) to increase their utility. We studied the tyrosinase-inhibition activity (activity test) and structural changes (circular dichroism) of tyrosinase with ED and plasma activated eugenol derivatives (PAED) in a cell-free environment.

Photodynamic Anticancer Activities of Multifunctional Cobalt Ferrite Nanoparticles in Various Cancer Cells.

To develop novel multifunctional magnetic nanoparticles (MNPs) with good magnetic properties, biocompatibility, and anticancer activities by photodynamic therapy (PDT), we synthesized multifunctional cobalt ferrite (CoFe2O4) nanoparticles (CoFe2O4-HPs-FAs) functionalized by coating them with hematoporphyrin (HP) for introducing photo-functionality and by conjugating with folic acid (FA) for targeting cancer cells. We evaluated the activities of the CoFe2O4-HPs-FAs by checking magnetic resonance imaging (MRI) in vitro, its biocompatibility, and photodynamic anticancer activities on FA receptor (FR)-positive and FR-negative cancer cell lines, Hela, KB, MCF-7, and PC-3 cells, to use for clinical applications. In this study, we have demonstrated that the CoFe2O4-HPs-FAs have good MRI and biocompatibility with non-cytotoxicity, and remarkable photodynamic anticancer activities at very low concentrations regardless of cell types.

Controlling conductivity of carbon film for L-929 cell biocompatibility using magnetron sputtering plasmas.

As a material of current interest compatible with many living organisms, carbon has received considerable attention for applications in medicine. To improve and investigate the performance and applications of diamond-like carbon (DLC) films for implantable bio-organs, it is important to optimize the synthesis process from the original deposition conditions to control the characterization of DLC. Simultaneously, it is necessary to develop new techniques and processes that yield DLC films with stronger adhesion to the substrate and better biocompatibility.

Optical properties of some novel 2,5-disubstituted 1,3,4-oxadiazole derivatives and their application as an efficient cell staining azo dyes.

A series of six 2,5-disubstituted 1,3,4-oxadiazole derivatives with various length of conjugation have been synthesized and their optical properties including UV-visible absorption spectra, fluorescence emission spectra, molar absorption co-efficient, Stokes shift and the relative fluorescence quantum yield were measured in a variety of organic solvents. Correlation of the absorption spectra and fluorescence emission response of the 2,5-disubstituted 1,3,4-oxadiazole derivatives with the substituent effect revealed that the optical response can easily be tuned toward red shift by increasing conjugation length. The synthesized compounds were further employed in bioimaging assay in order to investigate their potential as an efficient cell staining agent using L-929 cells under confocal fluorescence microscope which showed scrupulous cell permeability and no toxicity as assessed by MTT assay.

The smart 2-(2-fluorobenzoyl)-N-(2-methoxyphenyl)hydrazinecarbothioamide functionalized as Ni(II) sensor in micromolar concentration level and its application in live cell imaging.

In recent years, fluorescent probes for the detection of environmentally and biologically important metal cations have received extensive attention for designing and development of fluorescent chemosensors. Herein, we report the photophysical results of 2-(2-fluorobenzoyl)-N-(2-methoxyphenyl) hydrazinecarbothioamide (4) functionalized as Ni (II) sensor in micromolar concentration level. Through fluorescence titration at 488 nm, we were confirmed that ligand 4 showed the remarkable emission by complexation between 4 and Ni (II) while it appeared no emission in case of the competitive ions (Cr(3+), Fe(2+), Co(2+), Ba(2+), Cu(2+), Ca(2+), Na(+), K(+), Cu(+), Cs(+)).

Facile synthesis, cytotoxicity and bioimaging of Fe(3+) selective fluorescent chemosensor.

The designing and development of fluorescent chemosensors have recently been intensively explored for sensitive and specific detection of environmentally and biologically relevant metal ions in aqueous solution and living cells. Herein, we report the photophysical results of alanine substituted rhodamine B derivative 3 having specific binding affinity toward Fe(3+) with micro molar concentration level. Through fluorescence titration at 599nm, we were confirmed that ligand 3 exhibited ratiometric fluorescence response with remarkable enhancement in emission intensity by complexation between 3 and Fe(3+) while it appeared no emission in case of the competitive ions (Sc(3+), Yb(3+), In(3+), Ce(3+), Sm(3+), Cr(3+), Sn(2+), Pb(2+), Ni(2+), Co(2+), Cu(2+), Ba(2+), Ca(2+), Mg(2+), Ag(+), Cs(+), Cu(+), K(+)) in aqueous/methanol (60:40, v/v) at neutral pH.