Sudhir Kumar Paidesetty

Chitosan and folic acid dual-functionalized morin-reduced gold nanosystems exhibit multifunctionalities to tackle critical clinical challenges, like triple-negative breast cancer and antimicrobial resistance.

1. The global rise of antimicrobial resistance (AMR), a phenomenon first highlighted over four decades ago by Stanley Falkow, has now escalated into one of the most formidable global health threats...

An efficient synthesis of a series of 4‐phosphorylated‐2 H ‐chromenes has been developed via one‐pot multicomponent reaction of salicylaldehyde, β ‐nitrostyrene, and H ‐phosphonates/ H ‐phosphine oxide using DABCO as a base, delivering the desired products within a short reaction time of 5–20 min. This method demonstrates broad substrate scope and affords excellent yields ranging from 70%–92%. The resulting compounds were characterized by ¹ H, ¹³ C, and ³¹ P NMR and HRMS analysis. The compounds were evaluated for their in vitro antibacterial activity against three pathogenic bacterial strains E. coli , S. aureus , and K. pneumoniae . Among all the tested compounds, 4p and 4q showed antibacterial activity comparable to the standard antibiotic novobiocin against all tested strains with corresponding MIC values of 2 µg/mL for each. Additionally, in silico molecular docking studies revealed compound 4s has strong binding affinity of −10.2 kCal/mol against S. aureus and compound 4j exhibited a docking score of ‐9.0 kCal/mol against E. coli . Further DFT analyses of compounds 4c , 4j , 4p , 4q , 4o, and 4t were performed to elucidate the electronic stability. Owing to its operational simplicity, high efficiency and metal‐free nature, this protocol provides a valuable synthetic platform for accessing novel phosphorus‐containing heterocycles, which may hold potential for future drug discovery.

Nitrogen-bearing heterocycles have been fundamental scaffolds in drug discovery, contributing significantly to the design and development of therapeutic agents since the inception of modern medicinal chemistry. Among them, imidazolones have shown notable therapeutic relevance, particularly in oncology, antimicrobial resistance (AMR), and inflammation, yet they remain relatively underexplored. Nevertheless, the significant therapeutic and clinical efficacy of imidazolone-bearing drugs, such as Nilutamide, Irbesartan, and Leucettinib-21, in anticancer, antihypertensive, and neurotherapeutic applications has stimulated increasing interest in imidazolone chemistry and its medicinal potential. This review systematically discusses the major synthetic strategies, structure–activity relationships, and mechanistic principles governing the biological activity of imidazolones. Particular emphasis is placed on their rapidly expanding role as anticancer agents targeting enzymes and signaling proteins such as carbonic anhydrases, epidermal growth factor receptors (EGFR), Bcl-2 protein family, and checkpoint kinases, along with their potential applications in antimicrobial and anti-inflammatory therapies. Furthermore, the review highlights the complementary roles of computational modeling and biological evaluation in understanding the interactions of imidazolone-bearing compounds with various microbial and cancer-related receptors. These integrated studies reveal their ability to engage multiple biological targets and validate their observed pharmacological activities. The convergence of in silico predictions with experimental findings offers valuable guidance for the rational development of imidazolone-based therapeutics. Overall, this review emphasizes imidazolones as promising scaffolds with significant potential for future drug discovery and development.

Alzheimer’s disease (AD) is a global concern. Conventional FDA-approved drugs mostly provide symptomatic relief but largely fail to address the underlying pathophysiology of AD. Further, chronic use of prescribed anti-AD drugs causes unpredictable, countless side effects, which thus evokes exploration for novel, safer, nontoxic, affordable, yet potent alternative modalities. Among various predicted pathophysiological hall marks in the progression of AD, aberrant histone acetylation has been identified as one of the major culprits, which leads to dysregulated gene expression and gradual neuronal degeneration. Thus, histone acetyl transferase (HAT) inhibitors are considered lucrative anti-AD agents. Active phyto constituents in recent times have occupied the center stage in addressing challenging neurodegenerative disorders in place of routine drug therapy. Garcinol (GL), a phytoactive constituent from Garcinia indica, possesses potent HAT inhibitory effect. Reports show that GL exhibits profound antioxidant, anti-inflammatory, anticancer, and neuroprotection effects. Neuroprotection of GL could be attributed to its ability to reduce oxidative stress and modulate important signaling pathways involved in neuronal degeneration. Present review unveils potentiality of HAT inhibitors in improving memory functions and neuroprotection; with a special focus on GL. Mechanical insights into activity of GL in ameliorating neurodegeneration have been discussed with rationalized evidence of various preclinical reports. Side by side, a portion has been devoted to update the trending drug delivery approaches investigated in recent times for GL toward improved pharmacological performance.

The ornamental plant, Quisqualis indica L. has several pharmacognistic properties. The anti-bacterial activity of the plant extracts against common bacteria causing Urinary tract infections (UTIs) were determined. In this study, Quisqualis Indica L. plant samples were collected during the spring season from Kalahandi District of Odisha. The different solvent extracts of the medicinal plant, Q. indica were used for determining the anti-bacterial activity against human pathogenic micro-organisms isolated from samples of patients having UTIs. In all, urine samples from 110 patients having UTIs were analyzed. Antibiotic susceptibility of gram-positive and gram-negative bacterial isolates was studied. The Molsoft tool was used to identify the drug likeness score of each compound. Escherichia coli was observed in 57 %, Pseudomonas aeruginosa in 17 %, Staphylococcus aureus in 15 % and Klebsiella pneumoniae in 10 % of the samples. Escherichia coli was the most predominant bacteria isolated from UTIs. Seven bacterial strains were used in the study namely Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Streptococcus pyogenes and Acinetobacter baumannii. The extracts of Q. indica have significant anti-bacterial properties against Escherichia coli, Staphylococcus aureus, Klebsiella pneumoniae, Pseudomonas aeruginosa, Acinetobacter baumannii and Streptococcus pyogenes causing the UTIs. The compounds mainly Phytol, Trans-sequalene, Tocoferol, Vitamin-E-acetate and stigmasterol have higher drug likeness scores. Our study has reported the structural configuration of the extracts having higher drug-likeness score with a potential for future therapeutic drug against the UTIs. This study focusses on UTIs and the phytochemical analysis has been evaluated with drug likeness score.