Synthesis and Structure-Activity Relationship (SAR) Studies on New 4-Aminoquinoline-Hydrazones and Isatin Hybrids as Promising Antibacterial Agents.

In response to the escalating crisis of antimicrobial resistance (AMR), there is an urgent need to research and develop novel antibiotics. This study presents the synthesis and assessment of innovative 4-aminoquinoline-benzohydrazide-based molecular hybrids bearing aryl aldehydes () and substituted isatin warheads (), characterized using multispectroscopic techniques with high purity confirmed by HRMS. The compounds were evaluated against a panel of clinically relevant antibacterial strains including the Gram-positive , , and and a Gram-negative bacterial strain.

Design and Synthesis of Benzimidazole Carboxamide Cysteine Protease Inhibitors as Promising Anti-leishmanial Agents.

Introduction: More than 20 protozoan species of Leishmania are responsible for causing Leishmaniasis, an infection spread by blood-feeding phlebotomine sandflies. A narrow pool of drugs is currently available rendering the current drug stratagem to treat this infection . Development of novel, less toxic, and more effective regimens is thus a need of the hour.

Development and Evaluation of Bis-benzothiazoles as a New Class of Benzothiazoles Targeting DprE1 as Antitubercular Agents.

Benzothiazole-bearing compounds have emerged as potential noncovalent DprE1 (decaprenylphosphoryl-β-d-ribose-2'-epimerase) inhibitors active against . Based on structure-based virtual screening (PDB ID: 4KW5), a focused library of thirty-one skeletally diverse benzothiazole amides was prepared, and the compounds were assessed for their antitubercular activity against H37Ra. Most potent compounds and were further evaluated against the H37Rv strain by the microdilution assay method.

Aptasensor Integrated with Two-Dimensional Nanomaterial for Selective and Sensitive Electrochemical Detection of Ketamine Drug.

Ketamine is one of the most commonly abused drugs globally, posing a severe risk to social stability and human health, not only it is being used for recreational purposes, but this tasteless, odourless, and colourless drug also facilitates sexual assaults when it is mixed with drinks. Ketamine abuse is a threat for safety, and this misuse is one of the main uses of the drug. The crucial role of ketamine detection is evident in its contributions to forensic investigations, law enforcement, drug control, workplace integrity, and public health.

Wearable Electrochemical Glove-Based Analytical Device (eGAD) for the Detection of Methamphetamine Employing Silver Nanoparticles.

Illicit drug misuse has become a widespread issue that requires continuous drug monitoring and diagnosis. Wearable electrochemical drug detection devices possess the potential to function as potent screening instruments in the possession of law enforcement personnel, aiding in the fight against drug trafficking and facilitating forensic investigations conducted on site. These wearable sensors are promising alternatives to traditional detection methods.

Paper-Based Electrodes Decorated with Silver and Zinc Oxide Nanocomposite for Electro-Chemical Sensing of Methamphetamine.

We present the development of an electrochemical paper-based analytical device (ePAD) for the detection of methamphetamine. Methamphetamine is a stimulant that young people use as an addictive narcotic, and it must be detected quickly since it may be hazardous. The suggested ePAD has the advantages of being simple, affordable, and recyclable.

Deciphering the Precise Target for Saroglitazar Associated Antiangiogenic Effect: A Computational Synergistic Approach.

Antidiabetic drugs that have a secondary pharmacological effect on angiogenesis inhibition may help diabetic patients delay or avoid comorbidities caused by angiogenesis including malignancies. In recent studies, saroglitazar has exhibited antiangiogenic effects in diabetic retinopathy. The current study investigates the antiangiogenic effects of saroglitazar utilizing the chicken chorioallantoic membrane (CAM) assay and then identifies its precise mode of action on system-level protein networks.

Design, synthesis, characterizing and DFT calculations of a binary CT complex co-crystal of bioactive moieties in different polar solvents to investigate its pharmacological activity.

Imidazole (IM) and salicylic acid (SA) have a significant class among the medical compound. These are widely used as topical drugs like antifungal, antibacterial, anticancer, immunosuppressive agent, etc. These two bioactive organic moieties are combined by a weak hydrogen bond formed by hydrogen transfer.

A review on Japanese Encephalitis virus emergence, pathogenesis and detection: From conventional diagnostics to emerging rapid detection techniques.

The virus known as Japanese Encephalitis (JEV) is among the common viral persisting Encephalitis caused by Flavivirus around the Globe, especially in Southeast Asian nations. JEV may be a leading reason for neurological illness in humans, with an estimated 70,000 human cases and 10,000 fatalities per annum. The conventional methods like PRNT (Plaque Reduction Neutralization Test), ELISA (Enzyme-linked immunosorbent assay) RT-PCR (reverse transcription-polymerase chain reaction), and virus isolation are few commercial tests being availed these days, but they have a variety of drawbacks, including being extremely expensive, time-consuming, and requiring expertise.

Comparative genomic analyses of Bacillus subtilis strains to study the biochemical and molecular attributes of nattokinases.

The present research work explores the Nattokinase (NK) producing capacity of five Bacillus subtilis strains (MTCC 2616, MTCC 2756, MTCC 2451, MTCC 1427, and MTCC 7164) using soybean varieties as substrate under solid-state fermentation conditions. Subsequently, the biochemical attributes of NKs were analyzed. Soybean variety didn't affect the production of NK to a significant extent; however, the five strains differed substantially for their NK producing capacity.

Antimicrobial activity of different plants extracts against Staphylococcus aureus and Escherichia coli.

Background: Microbial pathogens, mainly bacteria, are a major cause of food spoilage resulting in several foodborne diseases. Food spoilage can be prevented by the application of chemical preservatives in the food industry but such process has harmful effects on human health and causes the introduction of chemicals in several food chains, leading to toxicity and long-term complications. Due to such adverse effects, the need to find natural preservatives that are safer to use, effective and less complicated is increasing.

Resveratrol loaded nanoparticles attenuate cognitive impairment and inflammatory markers in PTZ-induced kindled mice.

Resveratrol has been found to exert protective effects in neurological disorders, including epilepsy. However, its poor bioavailability and difficulty in reaching the brain's targeted location reduce resveratrol's efficacy substantially. The side effects due to the higher concentration of drugs are another matter of concern.

Synthesis, spectroscopic characterization, antimicrobial activity, molecular docking and DFT studies of proton transfer (H-bonded) complex of 8-aminoquinoline (donor) with chloranilic acid (acceptor).

The proton transfer complex has been synthesized by mixing 1:1 ratio of 8-aminoquinoline (donor) and chloranilic acid (acceptor) in methanol. FTIR, C NMR, H NMR, Powder XRD and UV-visible studies confirmed the formation of the newly synthesized compound. These methods ascertain that cations and anions combine to form weak hydrogen bonds as N-H----O.

Optimization of Protein Isolation and Label-Free Quantitative Proteomic Analysis in Four Different Tissues of Korean Ginseng.

Korean ginseng is one of the most valuable medicinal plants worldwide. However, our understanding of ginseng proteomics is largely limited due to difficulties in the extraction and resolution of ginseng proteins because of the presence of natural contaminants such as polysaccharides, phenols, and glycosides. Here, we compared four different protein extraction methods, namely, TCA/acetone, TCA/acetone-MeOH/chloroform, phenol-TCA/acetone, and phenol-MeOH/chloroform methods.

Protein PE6 (Rv0335c), a Novel TLR4 Agonist, Evokes an Inflammatory Response and Modulates the Cell Death Pathways in Macrophages to Enhance Intracellular Survival.

() is an intracellular pathogen that exploits moonlighting functions of its proteins to interfere with host cell functions. PE/PPE proteins utilize host inflammatory signaling and cell death pathways to promote pathogenesis. We report that PE6 protein (Rv0335c) is a secretory protein effector that interacts with innate immune toll-like receptor TLR4 on the macrophage cell surface and promotes activation of the canonical NFĸB signaling pathway to stimulate secretion of proinflammatory cytokines TNF-α, IL-12, and IL-6.

Boron Doped Carbon Quantum Dots: Turn-Off Fluorescent Probe for Dopamine Detection.

In this report, Boron-doped carbon quantum dots (BCQD, size = 2.3 nm) were fabricated by modified hydrothermal carbonization method by one-pot synthesis using phenyl boronic acid as the common precursor that provided seed for the formation of carbon quantum dots as well as the dopant. These quantum dots exhibited excellent properties including aqueous dispersibility, strong fluorescence emission, good environmental stability, highselectivity and sensitivity towards the neurochemical, dopamine even in the absence of any linker or functionalizing agents.

Exploring interaction dynamics of designed organic cocrystal charge transfer complex of 2-hydroxypyridine and oxalic acid with human serum albumin: Single crystal, spectrophotometric, theoretical and antimicrobial studies.

As human serum albumin (HSA) being the most abundant blood protein involved in the role of transport of molecules (drugs), we have designed HSA binding organic charge transfer complex between 2-hydroxypyridine (donor) and oxalic acid (acceptor) showing antimicrobial activities. The type of interactions between HSA and synthesized complex at the molecular level was studied through fluorescence spectroscopy. Binding constant along with the type of quenching mechanism was shown through the Stern Volmer equation.

Synthesis, characterization, antimicrobial and DNA binding properties of an organic charge transfer complex obtained from pyrazole and chloranilic acid.

The chemistry of an organic charge transfer complex (CT complex) between pyrazole (donor) and chloranilic acid (acceptor) has been explored in ethanol at room temperature. The synthesized complex has been characterized by various techniques such as FTIR, NMR, Single crystal X-ray diffraction and UV-visible spectroscopy. These techniques indicate that the cation and anion are joined together by the weak hydrogen bonding.

Metabolic Profiling-Based Evaluation of the Fermentative Behavior of and for Soybean Residues Treated at Different Temperatures.

Soybean processing, e.g., by soaking, heating, and fermentation, typically results in diverse metabolic changes.

Multifunctional, fluorescent DNA-derived carbon dots for biomedical applications: bioimaging, luminescent DNA hydrogels, and dopamine detection.

Here, we describe the synthesis of 2-3 nm, hydrophilic, blue fluorescence-emitting carbon dots (C-Dots, made using a DNA precursor) by the hydrothermal route from the gelling concentration of 2% (w/v) DNA. These dots exhibited highly efficient internalization in pathogenic fungal cells, negligible cytotoxicity, good PL stability, and high biocompatibility, thus demonstrating their potential as nanotrackers in microbial studies. Bioimaging was performed using Candida albicans as the representative for microbial pathogens.

Design and synthesis of newer 1,3,4-oxadiazole and 1,2,4-triazole based Topsentin analogues as anti-proliferative agent targeting tubulin.

A set of two series of 1,3,4-oxadiazole (11a-n) and 1,2,4-Triazole (12a, c, e, g, h, j-n) based topsentin analogues were prepared by replacing imizadole moiety of topsentin through a multistep synthesis starting from indole. All the compounds synthesized were submitted for single dose (10 µM) screening against a NCI panel of 60-human cancer cell lines. Among all cancer cell lines, colon (HCC-2998) and Breast (MCF-7, T-47D) cancer cell lines were found to be more susceptible for this class of compounds.