Mini reviews in medicinal chemistry最新文献

{"title":"Emerging Role of Natural Products and Dietary Supplements in Major Depressive Disorder: Therapeutic and Mechanistic Insights.","authors":"Ankit Kumar Yadav, Bikash Kumar Sah, Faiz Ahmad, Vishal Jamwal, Sanjeev Kumar Sahu","doi":"10.2174/0113895575464832260917050501","DOIUrl":"https://doi.org/10.2174/0113895575464832260917050501","url":null,"abstract":"<p><strong>Introduction: </strong>Major Depressive Disorder (MDD) is the fourth highest cause of morbidity and mortality in the world, and its prevalence has grown significantly during the COVID-19 pandemic. The pathophysiology of the disorder is multifactorial, involving genetic, environmental, cellular, and molecular factors. Traditional pharmacotherapies are characterized by delayed action, inadequate response, and side effects, thus prompting studies of complementary or additional treatments. The review aims to provide a comprehensive evaluation of the therapeutic potential of natural products and dietary supplements in MDD, clarify their mechanism of action, and identify new and integrative approaches to treatment.</p><p><strong>Methods: </strong>A systematic search was conducted through July 2025 across various databases, including PubMed, Google Scholar, Web of Science, repositories of traditional integrated resources, local dissertations, and monographs. The key terms included major depressive disorder with a combination of phytomedicine, natural products, dietary supplements, phytoconstituents, therapeutic potential, and mechanisms of action.</p><p><strong>Results: </strong>The use of natural products and dietary supplements has emerged as a potential means to effectively treat MDD due to their ability to regulate dysregulated biochemical processes and mechanisms.</p><p><strong>Discussion: </strong>Natural compounds such as polyphenols, alkaloids, terpenoids, and essential fatty acids use a variety of cellular and molecular pathways to have an antidepressant effect, including augmenting neurotransmitter levels, modulating the hypothalamic-pituitary-adrenal axis, reducing neuroinflammation, and inhibiting oxidative damage. Dietary supplements also contribute to mood regulation by supporting neuronal integrity, modulating the gut-brain axis, and maintaining immune homeostasis. The overall evidence suggests that natural interventions can be used to supplement traditional pharmacotherapy and enhance treatment success.</p><p><strong>Conclusion: </strong>The review provides a framework for the cellular and molecular pathways underlying the antidepressant effects of various natural compounds and dietary supplements, therefore establishing a foundation for future investigation and clinical use.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-09-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149111631","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Anti-Inflammatory Mechanism, Disease Treatment, and Application Prospects of Aloe-Emodin.","authors":"Jiameng Wu, Yuanzhi Liu, Yuan He, Lingdan Wu, Yue Li, Hongfei Liao, Qihua Xu, Anan Wang","doi":"10.2174/0113895575501739260904105719","DOIUrl":"https://doi.org/10.2174/0113895575501739260904105719","url":null,"abstract":"<p><p>Inflammation represents a common pathological foundation for numerous diseases. However, current anti-inflammatory agents, including antibiotics, Non-Steroidal Anti-Inflammatory Drugs (NSAIDs), glucocorticoids, and biologics, are frequently associated with significant limitations such as drug resistance, adverse effects, and high costs. Natural products have emerged as promising alternatives. Aloe-emodin, an anthraquinone compound, has attracted increasing attention due to its notable anti-inflammatory potential. This review systematically consolidates current knowledge regarding the molecular mechanisms underlying the anti-inflammatory effects of aloeemodin, along with its therapeutic applications, pharmacokinetic profile, and safety considerations. Key findings indicate that aloe-emodin acts through multiple targets, primarily by inhibiting core inflammatory pathways, including nuclear factor kappa light chain enhancer of activated B cells (NF-κB), mitogen-activated protein kinase (MAPK), NOD-like receptor protein 3 (NLRP3), and Phosphoinositide 3-kinase/protein kinase B (PI3K/Akt). Additionally, it modulates oxidative stress, regulates immune cell function, and influences the expression of cell adhesion molecules. Preclinical evidence supports its efficacy against infectious and non-infectious origins. But the main obstacle to the clinical application of aloe-emodin is its low oral bioavailability and the highly variable metabolic processes in the body, which are regulated by various factors. Although its dosedependent hepatotoxicity, nephrotoxicity, and phototoxicity have been reported, comprehensive safety testing under long-term, repeated-use conditions is still lacking. The latest progress in structural optimization and the development of new drug delivery systems offer promising methods to overcome these problems. Therefore, aloe-emodin is a potent natural anti-inflammatory agent. To promote the development of its therapeutic application, future work should focus on conducting high-quality clinical studies and combining computational predictions with in-depth mechanism verification to systematically elucidate its complex action network.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-09-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149111613","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Oleandrin and PBI-05204 for Neuroprotection in Alzheimer's Disease, Parkinson's Disease, and Stroke: Preclinical Mechanisms, Blood-brain Barrier Penetration, and Clinical Translation Perspectives.","authors":"Teenu Pal, Prabhat Singh","doi":"10.2174/0113895575485020260907153210","DOIUrl":"https://doi.org/10.2174/0113895575485020260907153210","url":null,"abstract":"<p><strong>Introduction: </strong>Alzheimer's disease, Parkinson's disease, and ischemic stroke are increasingly becoming one of the major health concerns across the globe due to the scarcity of effective treatments for these conditions. Natural compounds like oleandrin and PBI-05204 that are extracted from Nerium oleander have been recognised for their promising qualities in the treatment and prevention of these conditions due to their ability to provide protection to the neurons in the brain.</p><p><strong>Methods: </strong>A systematic review was conducted to identify preclinical research articles related to oleandrin and PBI-05204 in the treatment of Alzheimer's disease, Parkinson's disease, and ischemic stroke. Searches were conducted on articles from January 2021 to March 2026 in Pub- Med/MEDLINE, Scopus, and Web of Science using the terms \"oleandrin,\" \"PBI-05204,\" \"Nerium oleander,\" \"blood-brain barrier,\" \"neuroprotection,\" \"Alzheimer,\" \"Parkinson,\" and \"stroke.\" Original in vitro or in vivo preclinical studies providing information on neuroprotective results, mechanistic information (BDNF, Nrf2-ARE, apoptosis, mitochondria), or information on blood-brain barrier permeability were included. Non-original articles (reviews, editorials), preclinical research not involving any neurobiological parameters, and articles in languages other than English were excluded.</p><p><strong>Results: </strong>Preclinical studies suggest that both oleandrin and PBI-05204 can diffuse across the BBB and provide neuroprotection. These molecules were shown to increase the expression levels of BDNF, promote ARE-dependent transcription, rehabilitate mitochondrial function, and regulate apoptosis. Though these results are highly hopeful, the major translational gap is in the ability to reproduce preclinical success in the clinical environment.</p><p><strong>Discussion: </strong>There is sufficient cellular-molecular evidence for the potential use of these compounds, namely oleandrin, as well as PBI-052040. Some challenges may arise when attempting to apply such observations as a new treatment modality at the clinical research stage. This is true for bioavailability, toxicity, and regulatory factors that need to be addressed.</p><p><strong>Conclusion: </strong>Oleandrin and PBI-05204 make for very interesting compounds to consider for their neuroprotective properties in the context of neurodegeneration. Although there is promise in the preliminary human data from these compounds, there are also significant translational hurdles that must be cleared before their final application for human benefit.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-09-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149111911","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Unveiling the Pharmacognosy of an Aerial Parasite: Scurrula cordifolia and the Transfer of Medicinal Potential from Host to Mistletoe.","authors":"Vishal Choudhary, Emmanuel F Freeman, Yash Kumar, Manvika Karnatak","doi":"10.2174/0113895575467861260908044401","DOIUrl":"https://doi.org/10.2174/0113895575467861260908044401","url":null,"abstract":"<p><p>Mistletoes are obligate hemi-parasitic angiosperms that establish complex ecological and physiological relationships with their forest hosts through specialized haustorial systems. To maintain nutrient flux, these parasites withstand more negative water potentials than their hosts, utilizing succulent leaves for strategic rehydration. Although root parasites have been extensively studied, the absorptive structures and host-parasite dynamics of the Loranthaceae family, the largest group of mistletoes, remain under-investigated. This study explores the genus Scurrula, specifically the less-studied species Scurrula cordifolia, to understand how host-specific environments dictate phytochemical diversity. Unlike terrestrial plants regulated by soil and climate, Scurrula species bypass the soil, siphoning water and organic precursors directly from host xylem and phloem. This results in host-dependent metabolite profiles and bioactivities; for instance, S. ferruginea parasitizing Tecoma stans exhibits significantly higher anti-inflammatory activity than that on Vitex negundo. Furthermore, S. parasitica can sequester host-specific cardenolides and triterpenoids from Nerium indicum. Despite their traditional medicinal use, rigorous toxicological profiles for these complex extracts are lacking, particularly regarding long-term safety and dose-dependent effects. Evolutionary trends within Loranthaceae suggest a transition from ancestral root parasitism to derived aerial habits. Current observations indicate that S. cordifolia is experiencing significant population declines due to hyperparasitism by Viscum loranthi, highlighting a precarious biological equilibrium. Given the scarcity of in vivo data and the unique host-selective nature of these parasites, S. cordifolia presents a critical domain for future pharmacological and ecological research.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-09-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149111904","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Targeted Protein Degradation via the Ubiquitin-proteasome System: Emerging Advances and Therapeutic Challenges of PROTACs.","authors":"Somnath D Bhinge, Ganesh Gadekar, Vrushabh Patil, Ramling Mali, Bahubali Patil","doi":"10.2174/0113895575486076260907143722","DOIUrl":"https://doi.org/10.2174/0113895575486076260907143722","url":null,"abstract":"<p><strong>Introduction/objective: </strong>Proteolysis-targeting chimeras (PROTACs) are an emerging therapeutic technology in medicinal chemistry that induces selective degradation of target proteins through the ubiquitin-proteasome system. This review aims to summarize recent advances in PROTAC design, mechanisms of action, therapeutic applications, clinical development, and emerging strategies for overcoming current limitations.</p><p><strong>Methods: </strong>A structured literature search was conducted using PubMed, Scopus, Web of Science, and Google Scholar for studies published between January 2010 and December 2025. Search terms included \"PROTACs,\" \"proteolysis-targeting chimeras,\" \"targeted protein degradation,\" \"E3 ligase,\" \"protein degradation,\" and \"PROTAC clinical trials.\" Studies addressing PROTAC design, mechanisms, medicinal chemistry, therapeutic applications, and clinical development were included. Articles unrelated to targeted protein degradation, duplicate publications, non-relevant studies, and publications lacking sufficient scientific information were excluded.</p><p><strong>Results: </strong>The literature indicates that PROTACs can achieve efficient and selective degradation of disease-associated proteins, offering advantages over conventional occupancy-based inhibitors. Advances in E3 ligase recruitment, linker optimization, bifunctional degrader design, photoactivatable PROTACs, and dual-target degraders have substantially expanded the potential of this platform. Several PROTAC candidates have progressed into clinical development, supporting their translational potential.</p><p><strong>Discussion: </strong>Despite significant progress, challenges remain, including poor solubility, limited oral bioavailability, pharmacokinetic constraints, tissue-specific delivery, and potential off-target effects. Computational modeling, personalized medicine, and improved drug-delivery systems may facilitate more rational and efficient PROTAC development.</p><p><strong>Conclusion: </strong>PROTACs represent a promising approach for targeted protein degradation and may expand the druggable proteome. Continued advances in medicinal chemistry, pharmacology, computational design, and delivery technologies are essential for translating PROTACs into effective clinical therapies.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-09-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149111881","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Cinnamic Acid-based Hybrid Molecules as Multitarget Therapeutic Agents for Cancer, Alzheimer's Disease, and Malaria: A Review.","authors":"Anshika, Navin Kumar Tailor","doi":"10.2174/0113895575495727260909051459","DOIUrl":"https://doi.org/10.2174/0113895575495727260909051459","url":null,"abstract":"<p><p>Molecular hybridization has emerged as a powerful medicinal chemistry approach for address the limitations of conventional single-target therapeutics, particularly in the treatment of complex, multifactorial diseases. This strategy involves integrating two or more pharmacologically active pharmacophores into a single molecular framework, enabling enhanced biological activity, multi-target interactions, and improved pharmacokinetic properties. Among the diverse scaffolds investigated for hybrid drug design, cinnamic acid has attracted considerable attention owing to its structural simplicity, synthetic accessibility, and broad spectrum of biological activities. The incorporation of cinnamic acid into hybrid molecules has generated a wide range of compounds with improved therapeutic potential and selectivity. The pharmacological effects of cinnamic acid hybrids are associated with the modulation of key enzymes, including α-glucosidase, α-amylase, and acetylcholinesterase, as well as important signaling pathways such as NF-κB, COX-2, iNOS, PI3K/Akt/mTOR, and MAPK/ERK. These molecular interactions contribute to their diverse biological activities and therapeutic applications. This review provides a comprehensive overview of recent developments in cinnamic acid-based molecular hybrids, emphasizing design strategies, structure- activity relationships, pharmacological properties, and underlying mechanisms of action. Particular attention is given to their anticancer, neuroprotective, and antimalarial therapeutic applications. Furthermore, the review critically examines the advantages and current challenges of cinnamic acid hybridization and highlights future research directions. Overall, cinnamic acid-based molecular hybrids represent a promising platform for the development of multifunctional therapeutic agents with enhanced efficacy and broader clinical potential.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-09-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149111636","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Natural Products in the Prevention and Treatment of Skin Photoaging: A Review of Mechanisms, Challenges, and Future Perspectives.","authors":"Yushan Fang, Yan Chen, Li Chang, Shihua Wang, Changqing Jiang, Yiwen Zhang, Xiaocui Shuai, Wenjing Xiao, Jianyou Shi, Yonghe Hu","doi":"10.2174/0113895575484159260904095057","DOIUrl":"https://doi.org/10.2174/0113895575484159260904095057","url":null,"abstract":"<p><p>Increased UV radiation exposure, driven by ongoing ozone layer depletion, has emerged as a critical environmental factor compromising skin integrity. Among its various deleterious effects, photoaging represents a major dermatological concern. To systematically outline the progress in this field, this study first employed bibliometric analysis to review the current research landscape of skin photoaging. The results identified China, South Korea, and the United States as the leading contributors, with keywords such as \"antioxidant activity\" and \"apoptosis\" remaining persistent hotspots in recent years. This indicates a shifting research focus towards elucidating oxidative stress mechanisms and developing antioxidant-based intervention strategies. Furthermore, this review summarizes the core biological mechanisms and signaling pathways underlying skin photoaging and provides a systematic elaboration on the multi-target mechanisms by which various natural plant extracts mitigate UV-induced damage. These protective actions involve mitigating oxidative stress, reducing inflammatory responses, facilitating DNA repair, and inhibiting Matrix Metalloproteinase (MMP) activity to prevent collagen breakdown. Additionally, they include modulating hyaluronic acid levels and supporting immune function. The limitations of traditional small molecules and emerging macromolecular compounds in practical applications are also discussed. Despite their potential, natural extracts face challenges such as complex composition, poor stability and bioavailability of active constituents, and a lack of clinical studies. Future research should prioritize investigating multi-component synergistic mechanisms, optimizing extraction and purification techniques, and, crucially, innovating delivery technologies to enhance bioavailability and advance the development and clinical translation of natural products for combating skin photoaging.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-09-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149111814","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Cinnamon-derived Phenylpropanoids against Candida: Multi-target Mechanisms and Medicinal Chemistry Perspectives.","authors":"Zhaoling Shi, Jiajia Lin, Yang Xie, Wenna Zhang, Kelong Ma","doi":"10.2174/0113895575493800260904064024","DOIUrl":"https://doi.org/10.2174/0113895575493800260904064024","url":null,"abstract":"<p><p>Invasive candidiasis, particularly caused by drug-resistant strains, has emerged as a significant contributor to morbidity and mortality among hospitalized patients worldwide, posing a serious public health challenge. With the rising resistance to conventional antifungal agents such as azoles and echinocandins, the search for novel, effective, and low-toxicity antifungal lead compounds from natural products has become increasingly urgent. Cinnamon (Cinnamomum spp.), an ancient spice and medicinal plant, is rich in active components, notably cinnamaldehyde, eugenol, and cinnamic acid, which exhibit broad-spectrum and potent inhibitory effects against various Candida species, including clinically resistant strains. This review provides a systematic and updated synthesis of the anti-Candida mechanisms of these cinnamon-derived bioactive constituents, offering three distinctive contributions. First, a medicinal chemistry perspective was integrated, summarizing structure-activity relationships and physicochemical limitations that guide rational lead optimization. Second, a multi-target antifungal network encompassing cell wall/membrane disruption, biofilm and hyphal inhibition, metabolic interference, oxidative stress, and transcriptional modulation was delineated. Third, basic research to clinical translation was bridged by reviewing advanced formulation strategies, including nanoparticles, liposomes, nanofibers, and gels, alongside earlyphase clinical trial data. This multi-level integration, from molecular targets to delivery systems to human studies, provides a unique and actionable roadmap for developing cinnamon-derived nextgeneration anti-Candida therapeutics.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-09-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149081517","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pharmacological Profile of Thymoquinone: From Cellular Pathways to Nutraceutical Potential.","authors":"Upagya Gyaneshwari, Kumari Swati, Anand Prakash, Brijesh Pandey","doi":"10.2174/0113895575456689260904070048","DOIUrl":"https://doi.org/10.2174/0113895575456689260904070048","url":null,"abstract":"<p><strong>Introduction: </strong>Food-derived biomolecules offer high safety, accessibility, and therapeutic potential. Nigella sativa, particularly its bioactive terpenoid Thymoquinone (TQ), exhibits various pharmacological profile, including antioxidant, anti-inflammatory, and anticancer properties. This review summarizes the mechanistic roles of TQ in disease modulation and evaluates its potential for nutraceutical and pharmaceutical development.</p><p><strong>Methods: </strong>A systematic search of Google Scholar, PubMed, Scopus, Web of Science, and SciFinder (1990-2025) identified studies on the mechanism of action of TQ in cellular pathways, such as Wnt and JAK/STAT, and in redox reactions, along with clinical/preclinical models. The keywords used as filters were: Thymoquinone, anticancer, antioxidant, Nigella sativa, hepatoprotectant, neuroprotectant, cardioprotectant, nephroprotectant, and COVID-19.</p><p><strong>Results: </strong>TQ effectively modulates cell cycle arrest, ROS, and apoptosis. Significant dosage variability (30 mg/kg/day to 5000 mg/kg/day) exists across models, where emerging evidence suggests TQdeficient plant parts are an underexplored resource for TQ biosynthesis.</p><p><strong>Discussion: </strong>TQ has high translational value as a non-toxic adjuvant to conventional therapies, potentially reducing chemotherapy side effects and improving metabolic outcomes. However, clinical adoption requires standardized dosing and improved bioavailability through novel formulation strategies.</p><p><strong>Conclusion: </strong>As a versatile lead compound for chronic disease management, future TQ research should prioritize standardizing dosage protocols, exploring alternative plant parts for optimize resource use, and developing high-bioavailability nutraceutical formulations to enhance therapeutic delivery.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-09-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149081520","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Exploring the Antimicrobial Potential of Benzimidazole-based Compounds in Medicinal Chemistry: Advances and Perspectives.","authors":"Rakesh Chandra Kalita, Shivani Sharma, Mukta Gupta","doi":"10.2174/0113895575472704260904095316","DOIUrl":"https://doi.org/10.2174/0113895575472704260904095316","url":null,"abstract":"<p><strong>Introduction: </strong>The urgent need for novel antimicrobials to combat antibiotic resistance highlights benzimidazole derivatives as highly promising candidates. Over the past decade, extensive research has focused on the therapeutic potential of benzimidazole-based scaffolds in various pathological conditions, including bacterial infections.</p><p><strong>Methods: </strong>This review compiles and analyses studies published between 2014 and 2025, highlighting the long history of these molecules in the treatment of various infectious diseases. It also deciphers the latest updates on marketed formulations of benzimidazole derivatives used in infections. Additionally, clinical trials evaluating their efficacy and safety are discussed. Data were extracted regarding synthetic strategies, biological activities, physicochemical properties, and clinical trials.</p><p><strong>Results: </strong>Numerous benzimidazole-based compounds have shown promising results in several in vitro and in vivo investigations. Furthermore, their distinct structural diversity allows for their optimization as antibacterial agents, making them attractive candidates for the development of targeted therapies against specific bacterial pathogens.</p><p><strong>Discussion: </strong>Benzimidazole presents a privileged scaffold suitable for chemical optimization and provides space for structure-guided drug design exploration. These compounds exhibit antibacterial potential via various possible mechanisms, including DNA topoisomerase inhibition, disruption of protein synthesis, and membrane integrity.</p><p><strong>Conclusion: </strong>Benzimidazoles and their derivatives demonstrate strong preclinical promise; however, continued structural modification and biological evaluation may advance and translate them into new drug interventions for clinical practice.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-09-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149081515","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}