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2000

Current Topics in Medicinal Chemistry - Volume 25, Issue 20, 2025

Volume 25, Issue 20

Volume 25, Issue 20, 2025

    • A Pharmacological Update of Oxadiazole Derivatives: A Review

      https://doi.org/10.2174/0115680266349715250122001314
      Background

      Recent advancements in the synthesis of novel heterocyclic compounds, particularly oxadiazole derivatives, have garnered significant interest due to their broad pharmacological activities. Despite the oxadiazole ring being a relatively small structure, its derivatives have shown considerable therapeutic potential across a range of diseases. These compounds have been explored for a variety of biological effects, including anti-inflammatory, anticonvulsant, hypoglycemic, antitubercular, anxiolytic, antimicrobial, antitumor, and anticancer properties. The growing issue of drug resistance has further fueled research into the therapeutic promise of oxadiazole-based compounds, particularly for their ability to target resistant diseases.

      Objective

      This review aims to highlight the pharmacological profiles of oxadiazole derivatives, with a focus on how structural modifications can enhance their activity against specific therapeutic targets. Additionally, the review seeks to explore strategies for overcoming resistance mechanisms associated with these compounds, underscoring their potential in addressing emerging drug-resistant diseases.

      Conclusion

      Oxadiazole derivatives represent a promising class of compounds with significant therapeutic potential, particularly in the face of increasing drug resistance. Their diverse pharmacological activities and ability to be structurally optimized for specific therapeutic targets position them as valuable candidates for further research. Continued exploration of oxadiazole derivatives, with an emphasis on overcoming resistance, may lead to the development of novel treatments for a variety of challenging diseases.

    • The Functional Mechanism and Structure-Activity Relationship of Antibacterial Peptides

      https://doi.org/10.2174/0115680266350153250121072651

      The escalating growth and global dissemination of antimicrobial resistance underscore the urgency for the discovery of innovative antimicrobial agents. Antibacterial Peptides (AMPs) have emerged as promising candidates, distinctly outperforming conventional antibiotics due to their mitigated propensity for resistance development, expansive antibiofilm activity, and capacity to favorably modulate host immune responses. Consequently, AMPs have garnered significant attention in medical research circles and are anticipated to serve as novel therapeutic alternatives in combating microbial infections, particularly those involving drug-resistant bacteria, thereby inaugurating a novel paradigm in treatment strategies. This comprehensive review delves into the intricate structural and physicochemical attributes of AMPs, providing a concise overview. It further examines the advancements and anticipated clinical trajectories of AMP research, with a pivotal focus on elucidating their antimicrobial mechanisms and the intricate interplay between structure and activity. The aim of this review is twofold: firstly, to enhance the scientific community's comprehension of the antimicrobial mechanisms and Structure-Activity Relationships (SAR) across all classes of AMPs; secondly, to address existing research gaps in the SAR of AMPs, thereby laying a solid foundation for future research endeavors and facilitating the development of these promising therapeutic agents.

    • Unveiling the Anticancer Potential of Phytocompounds: Pioneering Future Cancer Therapies

      https://doi.org/10.2174/0115680266354680250121154720

      Cancer epidemiological studies highlight the critical need for identifying better treatment options against cancer. Plants have been widely studied to obtain their efficacy as potent therapeutic agents to treat several diseases, including cancer. Interestingly, some phytocompounds, such as flavonoids, terpenoids, alkaloids, phenolics, and organosulphur compounds [OSCs], have been demonstrating their potential role in combating several pathologies, including the second most devasting disease, cancer, which contributes a significant portion of annual mortality cases. Several , , and investigations have recently established remarkable properties of phytocompounds such as antioxidant effects, induction of apoptosis, inhibition of metastasis, autophagy modulation, cell cycle regulation, and chemosensitization that lead to cancer suppression. This underscores the great potential of phytocompounds to contribute as an effective anticancerous drug for the prevention of cancer cases and advancement in cancer research. Therefore, comprehending the complicated mechanism involved in the anticancerous effects of phytocompounds against several carcinomas is crucial to establishing novel therapeutic strategies. Thus, this review tends to summarize the involvement of the most promising classes of phytompounds in cancer management and highlights several clinical trial data that demonstrate significant results in managing diverse carcinomas.

    • Roles of C/EBPβ/AEP in Neurodegenerative Diseases

      https://doi.org/10.2174/0115680266357822250119172351

      In recent years, an increasing number of studies have shown that increased activation of aspartic endopeptidases (AEPs) is a common symptom in neurodegenerative diseases (NDDs). AEP cleaves amyloid precursor protein (APP), tau (microtubule-associated protein tau), α-synuclein (α-syn), SET (a 39-KDa phosphoprotein widely expressed in various tissues and localizes predominantly in the nucleus), and TAR DNA-binding protein 43 (TDP-43), and promotes their aggregation, contributing to Alzheimer's disease (AD), Parkinson's disease (PD), Huntington's disease, multiple sclerosis (MS), amyotrophic lateral sclerosis (ALS), and frontotemporal dementia (FTD) pathogenesis. Abundant evidence supports the notion that CCAAT/enhancer-binding protein β (C/EBPβ)/AEP may play an important role in NDDs. Developing its small molecule inhibitors is a promising treatment of NDDs. However, current research suggests that the pathophysiological mechanism of the C/EBPβ/AEP pathway is very complex in NDDs. This review summarizes the structure of C/EBPβ and AEP, their major physiological functions, potential pathogenesis, their small molecule inhibitors, and how C/EBPβ/AEP offers a novel pathway for the treatment of NDDs.

    • WISP3/CCN6 Adipocytokine Marker in Patients with Non-alcoholic Fatty Liver Disease (NAFLD) and its Association with Some Risk Factors

      https://doi.org/10.2174/0115680266334590241217065614
      Introduction

      CCN6/WISP3 is a member of the CCN adipokines family that can exert multiple effects on metabolic pathways. So far, the function of CCN6 in the pathogenesis of NAFLD has not been known well. Hence, we aimed to examine CCN6 serum levels in patients with NAFLD compared to healthy individuals and its association with some risk factors for the first time.

      Methods

      This case-control study measured serum levels of CCN6, TNF-α, IL-6, adiponectin, and fasting insulin using ELISA kits in 88 NAFLD patients and 88 controls. In addition, other biochemical variables, including AST, ALT, lipid profiles, and FBG, were determined using an Auto analyzer instrument.

      Results

      A remarkable decrease in CCN6 levels was found in the NAFLD patients (1501.9543 ± 483.414 pg/ml) compared to the healthy group (1899.4856 ± 559.704 pg/ml, < 0.001). In NAFLD patients, a negatively notable correlation was observed between CCN6 and the levels of insulin ( = -0.278, = 0.011), HOMA-IR ( = -0.268, = 0.014), as well as TNF-α ( = -0.343, = 0.001). A remarkable association was found between CCN6 and the risk factor of NAFLD in the adjusted model for gender, age, and BMI with OR = 0.867 (95% CI, [0.806-0.931], < 0.001).

      Conclusion

      Our findings showed a significant reduction in CCN6 levels in the NAFLD patients compared to the healthy group, as well as the developing risk of NAFLD enhanced with the decrease of CCN6 levels.

    • Therapeutic Potential of Quercetin in Type 2 Diabetes Based on a Network Pharmacology Study

      https://doi.org/10.2174/0115680266361598250212030220
      Introduction

      Currently, there are pharmacological treatments for type 2 diabetes (T2D), but these are ineffective. Quercetin is a flavonoid with antidiabetic properties.

      Objective

      This research aimed to identify the molecular mechanism of Quercetin in T2D from network pharmacology.

      Methods

      We obtained T2D-related genes from MalaCards and DisGeNET, while potential targets for Quercetin were sourced from SwissTargetPrediction and Comparative Toxicogenomics databases. The overlapping genes were identified and analyzed using ShinyGO 0.77. Subsequently, we constructed a protein-protein interaction network using Cytoscape, conducted molecular docking analyses with SwissDock, and validated the results through molecular dynamics simulation in GROMACS.

      Results

      Quercetin is involved in apoptotic processes and in the regulation of insulin activity, estrogen, prolactin and EGFR receptor. The key driver genes , , , , , , and showed high concordance in the molecular docking study, and molecular dynamics showed stability between Quercetin and ESR2 and PIK3R1.

      Conclusions

      Our work helps to identify the molecular mechanism and antidiabetic effect of quercetin, which needs to be studied experimentally.

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