Current topics in medicinal chemistry最新文献

Background: Thiazole-based compounds have attracted considerable interest due to their potent antioxidant abilities, which are crucial for combating diseases associated with oxidative stress. Over the last decade, significant progress has been made in the development and evaluation of thiazole derivatives exhibiting improved antioxidant properties.

Objective: This review aims to provide a comprehensive overview of the antioxidant properties of thiazole-derived compounds established over the past decade, emphasizing their SAR (Structureactivity relationships), mechanistic understanding, and potential therapeutic applications.

Methods: A comprehensive evaluation of peer-reviewed research from 2016 to 2025 was conducted, with an emphasis on studies investigating the antioxidant properties of thiazole-based compounds. SARs were evaluated to assess the effects of various substituents on antioxidant activity. Investigations into the mechanism were done further to understand the contribution of thiazole moieties in antioxidant activity.

Results: Various thiazole derivatives exhibited remarkable radical scavenging ability, frequently outperforming standard antioxidants. Structural characteristics including electron-donating substituents, catechol-containing scaffolds, and Schiff-base frameworks significantly improved activity. Metal complexes and hybrid structures enhanced the efficiency of electron transfer and the stability of radical intermediates.

Discussion: The findings indicate that thiazole derivatives exhibit antioxidant properties via synergistic structural and electronic characteristics that promote hydrogen-atom transfer along with single- electron transfer mechanisms. The integration of heterocyclic hybrids and metal coordination represents a promising strategy for the development of next-generation antioxidant agents characterized by enhanced stability and biological significance.

Conclusion: Over the last ten years, there have been significant advances in the development of thiazole-based antioxidants, including various derivatives exhibiting potent free radical scavenging capabilities. The results highlight the therapeutic efficacy of thiazole scaffolds in addressing diseases associated with oxidative stress. Future studies should focus on improving bioavailability and in vivo efficacy to facilitate the translation of these results into clinical applications.

Introduction: This study evaluates the antibacterial activity of zinc oxide nanoparticles dispersed in a polyvinylpyrrolidone solution (ZnO-NPs-PVP) synthesized using a green method based on corn starch.

Methods: The ZnO-NPs are characterized using Fourier Transform Infrared Spectroscopy (FT-IR), Transmission Electron Microscopy (TEM), Ultraviolet-Visible Spectroscopy (UV-vis), and Dynamic Light Scattering (DLS). The antibacterial efficacy of ZnO-NPs-PVP is assessed against the Gram-negative bacterium Pseudomonas aeruginosa by evaluating reductions in cell viability.

Results: FT-IR analysis reveals peaks typical of ZnO around 500 cm⁻¹, UV-vis spectroscopy shows a characteristic absorption band at 372 nm. TEM analysis indicates an average particle diameter of 23 nm, DLS reporting larger sizes (35 nm) due to the use of PVP as a dispersant. ZnO-NPs-PVP reduces bacterial viability by 3.75 log10 CFU/mL compared to the control. The antibacterial activity is concentration-dependent, with a 50% reduction in metabolic activity observed at 15 μg/mL. The SEM analysis shows the formation of pores in the bacterial cell wall, leading to intracellular component leakage and cell death.

Discussion: ZnO-NPs-PVP could serve as an effective alternative to conventional antibiotics, particularly in the context of increasing antimicrobial resistance.

Conclusion: The findings demonstrate that ZnO-NPs-PVP exhibits significant antibacterial activity and potential for use in antimicrobial treatments. Its ability to disrupt bacterial membranes and reduce metabolic activity suggests its utility as a promising candidate for future biomedical applications.

Introduction: The combinational chemo-herbal therapy effectively suppresses tumors and reduces their chemoresistance.

Objective: This study evaluated the anti-cancer and anti-tumor immunity properties of a chemoherbal therapy combination of Curcumin (Cur), Ginger (Gin), Clove (Clov), Ginger (Gin), and Amygdalin (Amyg) with Doxorubicin (DOX) against the Ehrlich Ascites Carcinoma (EAC) cell line.

Methods: The study examined the anti-tumor effects of herbal extracts from Cur, Gin, Clov, and Amyg alone and with DOX against EAC using the MTT assay. It evaluated anti-cancer and antitumoral immunity, cell counts, growth rates, and apoptosis of EAC cells, phenotypic expression of T lymphocytes (CD4+T and CD8+T) and natural killer (NK) cells, splenocyte and leucocyte counts, as well as Liver and kidney functions in EAC-challenged mice treated with extracts from Cur, Gin, Clov, and Amyg alone and with DOX.

Results: Chemo-herbal therapy using extracts of Cur, Gin, Clov, and Amyg combined with DOX showed significant anti-proliferative effects on EAC in vitro. In vivo, this combined treatment in tumor-challenged mice reduced EAC cell proliferation by decreasing cell counts and increasing apoptosis rates. Furthermore, it enhanced the expression of CD4+T and CD8+T lymphocytes and NK cells, while slightly increasing total leukocyte counts, neutrophils, and monocytes, but reducing total lymphocytes and eosinophils. Additionally, the combination therapy mitigated EAC-induced liver and kidney damage, restoring normal organ function.

Discussion: The integration of herbal extracts derived from Cur, Gin, Clov, and Amyg with the chemotherapy drug DOX may improve the effectiveness of chemotherapy in combating tumors and strengthen the immune response of the host against cancer.

Conclusion: Chemo-herbal therapy combining Cur, Gin, Clov, and Amyg with DOX may improve anti-tumor effects, enhance immune response, and reduce chemotherapy side effects, but requires additional in vivo studies for validation.

Dermatomyositis (DM) is a multifaceted autoimmune disorder arising from immune dysregulation and pathogenic (bacterial/viral) infections. The current therapeutic framework predominantly employs glucocorticoids, monoclonal antibodies, and immunosuppressive agents as first-line treatments. Nevertheless, there remains a critical need to develop novel targeted therapies that offer enhanced efficacy and reduced toxicity. This review comprehensively analyzes recent advances in small-molecule drug discovery for DM. Analyzing the Structure-Activity Relationship (SAR) of small molecule inhibitors and integrating the latest patents, this review combines both molecular design and clinical evidence with therapeutic strategies to point the way to the development of highly selective small molecules that target DM, a complex autoimmune disease, and ultimately contribute to the improvement of patients' prognosis and quality of life.

Heterocyclic compounds constitute a diverse and indispensable class of molecules, particularly in the pharmaceutical area, which represent a rich source of potential anticancer agents. Their distinctive structural features enable a wide range of biological activities, making them crucial for drug development. Heterocyclic compounds containing pyrrole, furan, thiophene, oxadiazole, coumarin, or benzimidazole rings have demonstrated activity against various cancer cell lines. In this study, we have reviewed and summarised various types of heterocyclic moieties for their anticancer activity. Heterocyclic compounds can interact with DNA, inhibiting its replication and transcription, ultimately leading to cell death. Currently, several drugs, including doxorubicin, 5- fluorouracil, and methotrexate, are active against various types of cancer. In this regard, research is being conducted to enhance their therapeutic effects and minimize their side effects. For a future perspective, there remains a need to explore newer anticancer agents, with heterocyclic compounds continuing to be a center of attention. Heterocyclic compounds can interfere with signaling pathways involved in cell proliferation, differentiation, and apoptosis, thereby disrupting the cancer phenotype and serving as a key structural feature of many anticancer drugs currently available on the market.

Introduction: The genus Allamanda (Apocynaceae), comprising approximately 16 species distributed in tropical and subtropical regions, is widely used in Southeast Asian and South American traditional medicine. Rich in terpenoids, flavonoids, and phenolics, it exhibits broad pharmacological potential. This review provides a comprehensive summary of the ethnobotany, phytochemistry, and therapeutic relevance of Allamanda to guide future research and drug development.

Methods: An extensive literature survey was conducted up to May 2025 using databases including SciFinder, PubMed, Scopus, and Google Scholar by using keywords such as Allamanda, Phytochemistry, Pharmacological activity, and Ethnobotany.

Results: Across the genus, a total of 209 compounds have been reported, predominantly terpenoids, followed by phenolics and volatiles. Preclinical studies have highlighted the antioxidant, antimicrobial, anti-inflammatory, antiviral, antifertility, wound-healing, and cytotoxic activities of Allamanda, supporting it as a promising source of new therapeutics.

Discussion: The rich phytochemical profile and broad pharmacology position Allamanda as a valuable ethnomedicinal resource with potential for modern drug discovery. However, the majority of studies are limited to preclinical studies, with minimal clinical validation and restricted species diversity. Future research should focus on chemical profiling, clinical trials, and safety assessment.

Conclusion: Allamanda offers a diverse array of bioactive compounds with significant pharmacological relevance. By integrating traditional uses with scientific evidence, this review highlights the potential of ethnomedicine in bridging the gap between traditional and modern pharmacology, while underscoring the need for future research on unexplored species.

Introduction: Postoperative complications are common issues that may arise from anesthetic drugs or surgical procedures. This study aimed to investigate the protective and therapeutic effects of ginsenosides on anesthesia-associated side effects and postoperative complications.

Methods: This study was conducted following the PRISMA 2020 guidelines. A comprehensive search was conducted across PubMed/MEDLINE, Scopus, Web of Science, Embase, and the Cochrane Library to identify relevant studies published prior to October 13, 2024. Predefined inclusion and exclusion criteria were applied, and duplicates were removed.

Results: Ginsenosides inhibit oxidative stress and enhance cognitive function by activating pathways such as phosphoinositide 3-kinase (PI3K)/Protein kinase B (PKB) (AKT)/glycogen synthase kinase-3 beta (GSK-3β), promoting neuroplasticity, alleviating oxidative stress, and modulating neuroinflammatory markers, as well as microglia and astrocytes. They help to maintain mitochondrial integrity, thereby reducing apoptosis and neurotoxicity caused by anesthetic agents. Ginsenosides also alleviate postoperative pain by modulating N-methyl-D-aspartate (NMDA) and suppressing inflammatory cytokines. They also improved neuropsychological problems by increasing Nerve Growth Factor (NGF) and Brain-Derived Neurotrophic Factor (BDNF). The anti-fatigue properties of ginsenosides are attributed to enhanced antioxidant activity, improved skeletal muscle metabolic function, and increased Adenosine Triphosphate (ATP) production.

Discussion: These results are consistent with prior studies demonstrating the neuroprotective effects of ginsenosides. Despite promising outcomes, the prevalence of animal studies and the absence of clinical data underscore the necessity for clinical validation and safety profiling in future research.

Conclusion: Preclinical evidence shows ginsenosides, particularly Rg1, Rb1, and Rg3, demonstrate promising protective and therapeutic effects against anesthesia-associated adverse effects and postoperative complications.

The employment of phytomolecules to treat cancer has become widespread in recent decades. Boswellic acids (BAs) are pentacyclic triterpenoids obtained from Boswellia oleo-gum resins. BAs are the primary active constituents of Boswellia resins and exhibit potent anticancer activity against numerous cancer cell lines. Consequently, they have garnered considerable attention as prominent anti-cancer agents. However, the pharmacokinetic characteristics of BAs, such as their low bioavailability and poor water solubility, pose significant barriers that limit their medicinal use. The aim of this review is to provide a thorough overview of the anticancer effects of BAs, along with their physiochemical parameters, pharmacokinetic profile, and structure-activity relationship (SAR). Furthermore, computational studies conducted on BAs to improve their therapeutic efficacy, relevant clinical studies evaluating BAs, the associated challenges, and future prospects have also been discussed. A systematic review of the literature was conducted to identify the effects of BAs in various cancers. The following databases were searched: PubMed, Web of Science, and Scopus, for prospective studies published between 2012 and 2025. Although BAs exhibit significant therapeutic potential, their clinical utility is limited by their pharmacokinetic profile. Focused studies on improved isolation techniques, the development of synthetic derivatives, and hybrid molecules are required to address these challenges. In addition, advancements in nanodrug delivery systems and computational studies are vital to overcome these barriers. Collectively, these strategies could prove helpful in establishing BAs as privileged scaffolds for developing anticancer drugs.

Breast cancer remains the second leading cause of cancer-related deaths worldwide, with mortality rates continuing to rise annually. While conventional treatments, such as surgery, chemotherapy, and radiotherapy, are available, they are not 100% effective and often damage healthy tissues, negatively impacting patients' quality of life. Naringenin, a promising phytonutrient, has demonstrated anti-cancer properties through various mechanisms that inactivate carcinogens. However, its therapeutic potential is limited by poor bioavailability and hydrophobic nature. Nanocarrier-based drug delivery systems, an application of nanotechnology, offer a promising solution to overcome these limitations. These systems enhance the solubility, circulatory half-life, and biodistribution of bioactive compounds like naringenin while reducing side effects. This innovative approach shows significant potential in improving breast cancer treatment outcomes.

Plant-powered nanotechnologies integrate the concepts of biological engineering and green synthesis to produce safe and environmentally friendly nanoparticles that address environmental and public health issues. Biological production, meanwhile, is a safe, biodegradable, as well as a sustainable method to create nanoparticles. Tabernaemontana divaricate, Calotropis gigantea (L.), Passiflora caerulea, Acorus calamus (rhizome), Cucurbita maxima (petals), Moringa oleifera (leaves), Piper nigrum, Ziziphus Spina Christi, Eucalyptus globulus, and Ziziphus oenoplia, etc., plants were among the medicinal flora used in the biological synthesis of Silver and Zinc oxide. Initially, phytochemical testing, scanning electron microscopy, energy-dispersive X-ray spectroscopy (EDS), X-ray diffraction, and electron microscopy were employed to characterize the greensynthesized Zinc oxide and silver nanoparticles. These medicinal floras have proven tremendous potential in the development of nanoparticles for several purposes in medicine, cosmeceuticals, food science and technology, water treatment and purification, environmental cleanup, and agriculture. This review paper highlights the characteristics of biologically produced Zinc oxide and Silver Nanoparticles and investigates the broad spectrum of plants that can be utilized in a single-phase, rapid protocol preparation approach that prioritizes green principles over conventional ones. These biologically friendly silver and zinc oxide nanoparticles have the potential to be very useful in the field of biomedicine, agriculture, cosmetics, water treatment, food science and technology, and the energy sector. The biomedicinal applications of green synthesised nanoparticles are particularly intriguing, with potential in drug delivery, bioimaging, antibacterial treatments, anti-Leishmanial properties, and cancer therapy. Compared to previous approaches, these nanoparticles provide benefits in terms of controlled administration, less toxicity, and increased therapeutic effectiveness. Future studies must concentrate on the development of affordable, non-hazardous, ecologically safe, and self-degradable nanoparticles to aid in the commercialisation of nanotechnology in agriculture, food, healthcare, and energy.