Jignesh Kamdar

In this study, we report a catalyst‐free Petasis Borono–Mannich approach for the efficient synthesis of novel 9 H ‐fluorene‐based alkyl‐amino derivatives with potential anti‐inflammatory activity. The reaction, involving 2‐fluorenecarboxaldehyde, various secondary amines, and substituted boronic acids, was optimized using 1,4‐dioxane and molecular sieves at 90°C, affording a series of compounds (4a–4o) in excellent yields. Biological evaluation via bovine serum albumin (BSA) denaturation assay revealed promising anti‐inflammatory activity, with compound 4o (IC ₅₀ = 13.02 µM) showing efficacy comparable to diclofenac sodium (IC ₅₀ = 12.11 µM). Structure–activity relationship (SAR) analysis indicated N ‐methylpiperazine and electron‐donating aryl boronic acids as key contributors to potency. Molecular docking against COX‐1 identified compound 4o as having the most favorable predicted docking score (−10.2 kcal/mol). Additionally, 100 ns molecular dynamics simulation of the lead 1EQG– 4o complex provided further insight into its conformational behavior and residue‐level flexibility under dynamic conditions. Preliminary in silico ADMET assessment indicated generally favorable absorption‐related properties across the series, while also identifying potential toxicity liabilities that require experimental validation.

Extremophilic prokaryotes survive salt, temperature, and pH extremes by coordinating stress-induced protein networks that preserve macromolecules, sustain energetics, and repair damage. This review integrates recent proteomics with functional genomics to resolve both network state and causality across halophiles, thermophiles, acidophiles, alkaliphiles, psychrophiles, and radiation-resistant prokaryotes. Quantitative proteomics maps condition-specific induction of chaperones, proteases, ion transporters, osmolyte pathways, DNA repair proteins, antioxidants, and envelope remodeling enzymes. Complementary perturbation genetics, functional genomics, and transcriptomics help to identify essential nodes and regulatory circuits underlying stress tolerance. In halophiles, compatible solute synthesis and Na⁺/H⁺ exchange couple to protein quality control and central metabolism, whereas many archaeal halophiles additionally rely on high intracellular salt and distinctive membrane chemistry. Thermophiles rely on heat-shock systems, ATP-dependent proteolysis, membrane adjustments, and redox balancing. Acidophiles maintain near-neutral cytosol via proton export and low-permeability membranes while linking iron handling to oxidative defense. Alkaliphiles use Na⁺-based bioenergetics, multi-subunit antiporters, and cell-wall modifications to retain protons. Psychrophiles emphasize cold-shock RNA chaperones, flexible enzymes, and cryoprotectants, whereas radiophiles combine exceptional DNA repair with strong antioxidant capacity. Across taxa, oxidative stress forms a cross-cutting axis that explains extensive regulon overlap and cross-protection. We synthesize network architecture, highlight conserved modules and lineage-specific solutions, and outline open questions in stress sensing, multi-stress integration, and the functions of uncharacterized proteins. These insights provide a framework for engineering robust biocatalysts and organisms for biotechnology and environmental applications.

We derived a new series of barbituric acid-1,2,3-triazole hybrids (9a–9j) using Cu(I)-catalyzed azide–alkyne cycloaddition, and traditional spectroscopic methods have been used to study them. The compounds were tested for their ability to kill cells in vitro by using the MCF-7 human breast cancer cell line and for their ability to stop the biological function of cyclin-dependent kinase 2 (CDK2). Biological findings indicated a moderate impact of phenyl ring substitution on activity. Compounds containing electron-withdrawing groups, especially 9g (4-CF ₃ ) and 9h (4-F), were very effective at inhibiting CDK2, with IC ₅₀ values of 3.12 and 4.20 µM, respectively. Compound 9e (4-Me) exhibited the maximum cytotoxicity against MCF-7 cells (IC ₅₀ = 2.02 µM), followed by compounds 9g and 9b. Structure–activity relationship research revealed that both electronic and hydrophobic effects at the para-position substantially affect activity. Molecular docking investigations corroborated these findings, illustrating advantageous interactions of active chemicals within the ATP-binding pocket of CDK2.

Stem rot of groundnut caused by Sclerotium rolfsii Sacc. is one of the major constraint to groundnut production in many countries. The fungus is ubiquitous, soil inhabitant and non-target. Screening of groundnut genotypes for resistance to stem rot under field conditions is complicated by the non-uniform spatial distribution of the pathogen. While development and maintenance of artificial sick plot with optimum inoculums load under field conditions are also difficult because of sensitivity of the pathogen to temperature, humidity, soil type, cropping system and host preference. In the present study, a screening technique under field conditions with high disease pressure has been reported. Twenty-five wild Arachis accessions and 178 F₃ progenies along with two parents were screened under pot and field conditions, respectively for resistance to stem rot. Two wild Arachis accessions and three F₃ lines were found resistant to stem rot with mortality less than 20% and 10%, respectively.

Extremophilic bacteria survive salt, temperature, and pH extremes by coordinating stress-induced protein networks that preserve macromolecules, sustain energetics, and repair damage. This review integrates recent proteomics with functional genomics to resolve both network state and causality across halophiles, thermophiles, acidophiles, and alkaliphiles, with targeted contrasts from psychrophiles and radiation-resistant bacteria. Quantitative proteomics maps condition-specific induction of chaperones, proteases, ion transporters, osmolyte pathways, DNA repair proteins, antioxidants, and envelope remodelling enzymes. Complementary perturbation genetics/functional genomics and transcriptomics help identify essential nodes and regulatory circuits underlying stress tolerance. In halophiles, compatible solute synthesis and Na+/H+ exchange couple to protein quality control and central metabolism. Thermophiles rely on heat-shock systems, ATP-dependent proteolysis, membrane adjustments, and redox balancing. Acidophiles maintain near-neutral cytosol via proton export and low-permeability membranes while linking iron handling to oxidative defence. Alkaliphiles use Na+-based bioenergetics, multi-subunit antiporters, and cell wall modifications to retain protons. Psychrophiles emphasize cold-shock RNA chaperones, flexible enzymes, and cryoprotectants, whereas radiophiles combine exceptional DNA repair with strong antioxidant capacity. Across clades, oxidative stress forms a cross-cutting axis that explains extensive regulon overlap and cross-protection. We synthesize network architecture, highlight conserved modules and lineage-specific solutions, and outline open questions in stress sensing, multi-stress integration, and functions of uncharacterized proteins. These insights provide a framework for engineering robust biocatalysts and organisms for biotechnology and environmental applications.

Identification of different strains of probiotic microorganisms is crucial for advancing applications in food and pharmaceutical companies. This study aimed to isolate and characterize Lactobacillus spp. from curd samples collected across various locations in Rajkot district to evaluate their probiotic potential. A total of 24 isolates were obtained and subjected to phenotypic assessments, including growth at different temperatures, pH levels, bile and NaCl salt tolerance, as well as catalase and oxidase activity, antibiotic susceptibility and cell surface hydrophobicity. The isolates predominantly exhibited characteristics consistent with Lactobacillus spp., with Lactobacillus acidophilus identified as the most prevalent. Notably, isolate SGG1 demonstrated robust phenotypic traits, including high hydrophobicity, acid and bile salt tolerance and resistance to selected antibiotics, indicating its suitability as a probiotic candidate The findings suggest that these Lactobacillus strains, particularly L. acidophilus, possess promising probiotic attributes, necessitating further in vivo investigations to confirm their health benefits and potential applications in food and pharmaceutical industries.

A series of indoline hybrids with amide and sulfonamide functionalities containing furan ( 6a–k ) and pyrrole ( 13a–k ) were synthesized through a multistep process with good yield. The final compounds were purified using reverse‐phase flash chromatography and characterized by FTIR, ¹ H NMR, ¹³ C NMR, LC–MS, and elemental analysis. These compounds were evaluated for their in vitro antibacterial activity against various bacterial strains, including Bacillus subtilis, Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli. Among the compounds tested, compound 6k and 13e exhibited the highest activity, demonstrating potency compared to the standard antibiotic drugs utilized. The antifungal activity of these newly synthesize compounds was also assessed in vitro against Aspergillus niger and Candida albicans, the results emphasized that compounds 6k and 13e displayed the highest activity, compared to the standard antifungal drug nystatin. Furthermore, in silico investigations of compounds 6a–k and 13a–k with E. coli DNA gyrase, using molecular docking and molecular dynamics simulations, revealed exceptional binding affinity of these derivatives to the protein's active site. Additionally, in silico ADMET analysis indicated favorable pharmacokinetic properties with no major toxicity concerns, highlighting their potential as effective antimicrobial agents.