{"title":"A Review of Antimicrobial Potential of Substituted Imidazole Scaffolds.","authors":"Vikas Verma, Pratibha Periwal, Sonia Rohilla, Meenakshi Bhatia, Vikramjeet Singh","doi":"10.2174/0113895575463489260825062510","DOIUrl":"https://doi.org/10.2174/0113895575463489260825062510","url":null,"abstract":"<p><p>The alarming rise of life-threatening microbial infections has intensified the search for novel broad-spectrum antimicrobial agents. Imidazole, a versatile nitrogen-containing heterocycle, has emerged as a privileged scaffold due to its diverse biological activities, including antibacterial, antifungal, and anticancer properties. Clinically important drugs such as Metronidazole, Ketoconazole, and Clotrimazole exemplify the therapeutic relevance of the imidazole core. Recent studies demonstrate that the antimicrobial potency of imidazole derivatives is strongly influenced by their substitution pattern. In particular, monosubstituted, disubstituted, trisubstituted, and tetrasubstituted imidazole frameworks exhibit distinct structure-activity relationships, where the nature, position, and number of substituents significantly modulate antibacterial efficacy, spectrum of activity, and target selectivity. This review systematically summarizes recent advances in substituted imidazole derivatives, highlighting how distinct substitution modes correlate with enhanced antibacterial and antifungal activities and providing strategic insights for the rational design of next-generation antimicrobial agents.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-09-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148945283","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}
Da Peng Wang, Zi Long Tan, Xiao Li Shen, Xu Hui Wang
{"title":"Precision Medicine in Prolactinomas: From Bench to Bedside.","authors":"Da Peng Wang, Zi Long Tan, Xiao Li Shen, Xu Hui Wang","doi":"10.2174/0113895575449555260825070815","DOIUrl":"https://doi.org/10.2174/0113895575449555260825070815","url":null,"abstract":"<p><p>Lactotroph adenomas (prolactinomas, PRLomas) are the most frequently diagnosed pituitary neuroendocrine tumors and originate from anterior pituitary lactotroph cells. Excess prolactin secretion is the defining feature and typically leads to reproductive/endocrine dysfunction; when lesions enlarge, symptoms related to local compression may also occur. In clinical practice, microadenomas are reported predominantly in women, whereas men more often present with macroadenomas, a distribution that may relate to differences in symptom recognition and time to diagnosis. Current mechanistic data support a multifaceted model in which estrogen-related signaling, inherited or acquired genetic/epigenetic alterations, and dysregulated pathways, including PI3K/AKT/mTOR and RAS/RAF/MEK/ERK, intersect to promote tumor growth and functional activity. Patients therefore present along a spectrum, ranging from hypogonadism, infertility, and sex-specific manifestations to visual compromise, cranial neuropathies, or hypopituitarism in advanced disease. Dopamine agonists (DAs), particularly cabergoline, remain the standard first-line therapy; however, endoscopic surgery is increasingly used in selected patients (e.g., wellcircumscribed microadenomas and carefully chosen macroadenomas in experienced centers). For aggressive, DA-resistant, or malignant PRLomas, temozolomide remains the main systemic salvage option, and immunotherapy is being explored in early-phase settings. A precision approach will likely depend on integrating molecular stratification with clinical behavior to individualize treatment sequencing and improve long-term control and quality of life.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-09-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148945329","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}
Ayush Jain, Chandana Majee, Ruchi Sharma, Rupa Mazunder
{"title":"Insight Into the Recent Advancements in Thiazolidinedione Derivatives as PPAR-γ Agonists for the Treatment of Type 2 Diabetes.","authors":"Ayush Jain, Chandana Majee, Ruchi Sharma, Rupa Mazunder","doi":"10.2174/0113895575484618260821093418","DOIUrl":"https://doi.org/10.2174/0113895575484618260821093418","url":null,"abstract":"<p><strong>Introduction: </strong>Thiazolidinediones, commonly known as glitazones, serve as a vital biological framework in the treatment of type 2 diabetes. This established class of medications works by lowering insulin resistance and improving the body's ability to utilize glucose in peripheral tissues. They achieve this by activating PPAR-γ, a PPAR subtype. Additionally, various hybrid PPAR- γ agonists have demonstrated multiple therapeutic effects, including antidiabetic activity. This review is designed to consolidate and evaluate current research regarding the therapeutic benefits and structure-activity relationship, synthesis, and both marketed and non-marketed thiazolidinedione analogues developed for treating type 2 diabetes over the past two decades.</p><p><strong>Methods: </strong>To achieve this objective, a comprehensive search was conducted across various academic and legal databases such as PubMed, ScienceDirect, Google Scholar, and so on. The process involved synthesizing data from original research manuscripts, review articles, and patent filings from 2016 to 2026, which were then critically analyzed.</p><p><strong>Result: </strong>The thiazolidinedione scaffold has been a key focus in research on biological activity and the synthesis of novel derivatives for managing type 2 diabetes, particularly in treating insulin resistance.</p><p><strong>Discussion: </strong>However, complications such as fluid retention, idiosyncratic hepatotoxicity, weight gain, and CHF associated with rosiglitazone and pioglitazone have limited their use. To improve efficacy and reduce side effects, various research groups have developed newer analogues.</p><p><strong>Conclusion: </strong>The potential of thiazolidinediones, regarding their chemical development and interaction with PPAR-γ receptors, is well known. Newer TZD analogues that offer enhanced safety and tolerability are anticipated to become widely accessible soon.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-09-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148945347","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":"Harnessing Synergy: A Review on the Synthesis and Bioactivity of Artemisinin-Isatin Hybrid Molecules.","authors":"Vishal Choudhary, Aanya Saini, Emmanuel F Freeman, Yash Kumar, Manvika Karnatak","doi":"10.2174/0113895575459849260822123712","DOIUrl":"https://doi.org/10.2174/0113895575459849260822123712","url":null,"abstract":"<p><strong>Introduction: </strong>To examine the design, synthesis, and pharmacological potential of novel artemisinin-isatin hybrid compounds as a strategy to overcome drug resistance and expand therapeutic applications beyond malaria.</p><p><strong>Methods: </strong>Researchers employed molecular hybridization techniques-specifically Cu-promoted azide-alkyne cycloaddition, etherification, and esterification-to covalently link modified isatin moieties to the artemisinin scaffold. These methods produced diverse series of triazole, two-carbon, and ester-tethered hybrids. The compounds were evaluated using MTT assays to determine biological activity against various cancer cell lines.</p><p><strong>Results: </strong>Pharmacological testing identified several potent hybrids: Hybrids 3c and 3d: Demonstrated efficacy against breast cancer lines comparable to the standard drug doxorubicin. Hybrid 5d: Showed significant anti-leukemic activity with an enhanced safety profile. SAR Analysis: Structure-activity relationship (SAR) data indicated that therapeutic effectiveness is highly dependent on the length of the alkyl linker (with two carbons being ideal) and specific modifications at the C-3 and C-5 positions.</p><p><strong>Discussion: </strong>The review discussed the preparation and biological activities of artemisinin and isatin hybrid molecules. It has been discussed that after the resistant reported against artemisinin, several approaches have been tried to improve the efficacy of drugs in the treatment of deadly diseases like malaria. It has been found that hybrids like artemisinin-1,2,3-triazole-isatin, dihydroartemisininisatin, two-carbon tethered artemisinin-isatin hybrids, ester tethered artemisinin-isatin hybrids, ester tethered artemisinin-isatin hybrids reported better efficacy. Also, the comparison between linkers showed that alkyl linkers provide more potency than 1,2,3- triazole linkers for artemisinin and isatin hybrids.</p><p><strong>Conclusion: </strong>Artemisinin-isatin hybrids represent a promising new class of pharmaceuticals that utilize synergy to target multiple cellular pathways. These hybrids offer a robust approach for treating complex diseases, including aggressive breast cancer and leukemia, while addressing the challenges of drug resistance.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-09-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148945320","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}
Pedro Alves Bezerra Morais, Lucas Inacio Dos Santos Ferreira, Jéssica Adalgisa Barbosa Silva, Gabriel Scudino Freitas, Lara Chaves de Freitas Ferreira, Elziane Favoreto Alves Firmino, Adilson Vidal Costa, Vagner Tebaldi de Queiroz, Heberth de Paula, Valdemar Lacerda Júnior
{"title":"Recent Progress in the Synthesis of Succinate Dehydrogenase Inhibitors: From Pyrazole-Coupled Carboxamides and Beyond.","authors":"Pedro Alves Bezerra Morais, Lucas Inacio Dos Santos Ferreira, Jéssica Adalgisa Barbosa Silva, Gabriel Scudino Freitas, Lara Chaves de Freitas Ferreira, Elziane Favoreto Alves Firmino, Adilson Vidal Costa, Vagner Tebaldi de Queiroz, Heberth de Paula, Valdemar Lacerda Júnior","doi":"10.2174/0113895575446683260811054954","DOIUrl":"https://doi.org/10.2174/0113895575446683260811054954","url":null,"abstract":"<p><p>A growing global population and increasingly stringent food-security demands, together with evolving challenges such as crop diseases, resistant weeds, and agrochemical-resistant pathogenic microorganisms, require new strategies to safeguard agricultural productivity. Succinate dehydrogenase (SDH, also known as complex II) participates in both the tricarboxylic acid cycle and the mitochondrial respiratory chain in pathogenic fungi, thereby affecting fungal metabolism and mitochondrial respiration. This enzyme has therefore been widely explored as a target in the search for new fungicides. Currently, 25 commercially available succinate dehydrogenase inhibitors (SDHIs) are used to protect economically important crops. The discovery of new agrochemicals is driven by the need to mitigate annual losses in agricultural productivity, estimated at approximately US$220 billion per year. This review summarizes advances in the synthesis of potent SDHIs over the last decade, including semisynthetic approaches and strategies combining carboxamide scaffolds with heterocyclic moieties based on bioisosterism, scaffold hopping, and molecular hybridization. The studies summarized here show that numerous hit compounds have recently been synthesized with EC50 values against several fungal strains and IC50 values for SDH inhibition that compare favorably with those of reference agrochemicals such as boscalid, thifluzamide, fluxapyroxad, fenfuram, and fluopyram. Finally, both established and emerging synthetic methods aimed at accelerating the generation of large compound libraries are increasingly supported by robust computational approaches, including 3D-QSAR and molecular dynamics simulations, to predict binding modes and provide structural insights for future investigations.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-09-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148945323","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":"Sponge Derived Macrolides (2000-2023): Chemical Diversity, Mechanistic Insights and Therapeutic Potential.","authors":"Afsona Khatun, Ritabrata Koley, Shaileyee Das","doi":"10.2174/0113895575459049260824150843","DOIUrl":"https://doi.org/10.2174/0113895575459049260824150843","url":null,"abstract":"<p><p>Macrolides, a class of antibiotics commonly used in clinical practice, have been derived from naturally occurring compounds found in marine sponges. This narrative mini-review covers the period from 2000 to 2023, focusing on the chemical, mechanistic insights, and therapeutic potential of 96 novel macrolide compounds isolated from marine sponge species. These metabolites have structurally intricate macrocyclic lactone structures, often featuring polyene chains, spiroketal systems, tetrahydropyran units, glycosidic components, and halogen substituents that enhance their biological efficacy and target selectivity. Sponge-derived macrolides exhibit significant cytotoxic, anticancer, antibacterial, antifungal, and anti-inflammatory properties, with several compounds showing nanomolar potency against drug-resistant cancer cell lines. Mechanistic studies identify various molecular targets, such as the control of microtubule dynamics, disruption of actin filaments, induction of mitochondrial-mediated apoptosis, suppression of protein synthesis, and regulation of the PI3K/Akt and MAPK signalling pathways. Recent trends in structure-activity relationships reveal that macrocycle size, conformational rigidity, stereochemical arrangement, and functional group distribution significantly affect potency and selectivity. Several sponge-derived macrolides and their synthetic analogues have notably progressed into preclinical evaluation, showing promising in vivo antitumor efficacy and enhanced pharmacokinetic profiles. Nevertheless, obstacles such as restricted natural availability, intricate structural characteristics, scalability issues in synthesis, and the need for enhanced safety margin optimization continue to hinder clinical translation. Ongoing advancements in total synthesis, semisynthetic modification, biosynthetic engineering, and formulation strategies are anticipated to expedite their movement towards marine drug development.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-09-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148945297","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}
Abhishek Maurya, Ashish Yadav, Saurabh Singh, Manjot Singh, Surendra Jatav, Shriyansh Srivastava, S K Abdul Rahaman, Rakesh Sahu
{"title":"Decoding Histamine Receptor Modulation: The Role of Heterocyclic Compounds in Next-generation Antihistaminic Drugs.","authors":"Abhishek Maurya, Ashish Yadav, Saurabh Singh, Manjot Singh, Surendra Jatav, Shriyansh Srivastava, S K Abdul Rahaman, Rakesh Sahu","doi":"10.2174/0113895575484983260821084406","DOIUrl":"https://doi.org/10.2174/0113895575484983260821084406","url":null,"abstract":"<p><p>The field of heterocyclic chemistry is a vital area of medicinal chemistry, characterized by notable dynamism that helps develop many physiologically active drugs. The extensive presence of heterocycles in drugs, natural products, and biological intermediates underscores their importance in the development of contemporary drugs. Histamine is an important endogenous biogenic amine with various physiological and immunological roles, including the inflammatory response, gastric acid secretion, neurotransmission, and immune regulation. The physiological effects of histamine are mediated by its interaction with four types of histamine receptors (H1, H2, H3, and H4). Histaminergic agents are of significant therapeutic importance due to their involvement in various disorders through dysregulated activity. Antihistamines have found applications in the management of problems related to the stomach, allergies, and certain neurodegenerative disorders. These drugs act by blocking histamine receptors. The first- and second-generation H1 antihistamines continue to play an important role in treating motion sickness, urticaria, and allergic rhinitis, as well as other conditions associated with these conditions. However, modern analogues of these drugs are much safer and do not cause any sedation. This review discusses the diversity of heterocycles in antihistaminic drugs, their interactions with receptors, their medicinal value, and the medicinal chemistry approaches that have paved the way for the development of such antihistamines.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-09-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148945296","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}
Phuong-Thuy T Phan, Thien-Phu H Luu, Khanh-Vy Nguyen, Tuan-Anh N Pham
{"title":"Structural Insights and Biological Activities of Salicylanilide-based Compounds: A Comprehensive Review.","authors":"Phuong-Thuy T Phan, Thien-Phu H Luu, Khanh-Vy Nguyen, Tuan-Anh N Pham","doi":"10.2174/0113895575494098260824152357","DOIUrl":"https://doi.org/10.2174/0113895575494098260824152357","url":null,"abstract":"<p><p>Salicylanilide-based compounds represent a versatile class of bioactive molecules with broad therapeutic potential. Originally developed as anthelmintic agents, these compounds have subsequently attracted considerable attention due to their diverse pharmacological activities, including antimicrobial, anticancer, anti-osteoclastogenic, anti-obesity, cardiovascular, and neuroprotective effects. In recent years, extensive medicinal chemistry efforts have focused on optimizing the salicylanilide scaffold to improve biological activity, target selectivity, and pharmacokinetic properties. This review provides a comprehensive overview of the therapeutic applications of salicylanilide derivatives, emphasizing recent advances in their medicinal chemistry, mechanisms of action, and structure-activity relationships (SARs). Analysis of available SAR data reveals several recurring trends across different therapeutic areas. Biological activity is frequently enhanced by electronwithdrawing substituents on the anilide ring, while the phenolic hydroxyl group often plays a critical role in target engagement, although its importance may vary depending on the pharmacological application. In addition, strategic scaffold modifications, including carbamate and thiocarbamate derivatization, prodrug approaches, heterocycle incorporation, and ring-fused analogues, have been successfully employed to improve potency, selectivity, solubility, and bioavailability. Collectively, the available evidence highlights the salicylanilide scaffold as a promising platform for the development of novel therapeutics. The SAR insights summarized in this review provide a valuable framework for the rational design and optimization of next-generation salicylanilide-based drug candidates and support further in vivo and clinical investigations of this scaffold.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-09-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148943957","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":"Unlocking Histone Deacetylase Inhibition with Chalcone Chemistry.","authors":"Ramya Savithri Kabekkodu, Shruthi Nayak, Ipshita Das, Yashaswini Reddy, Babitha Kampa Sundara","doi":"10.2174/0113895575478081260821091258","DOIUrl":"https://doi.org/10.2174/0113895575478081260821091258","url":null,"abstract":"<p><p>Chalcone, a prominent scaffold, is well recognized for its anticancer properties. The overexpression of epigenetic regulatory enzymes such as histone deacetylases (HDACs) has been associated with tumour progression and cancer development. The role of the chalcone scaffold in the inhibition of HDACs has been explored over the years. This study investigated the research progress reported on HDAC inhibition by compounds with a chalcone scaffold and evaluated their potential in medicinal chemistry. The research articles were sourced from multiple databases, such as SCOPUS, Google Scholar and PubMed, via the keywords 'chalcone', 'histone deacetylase inhibitor', 'HDACi', 'HDAC' and 'chalcone HDAC inhibitor'. The articles are classified into two main categories according to their structural features. First, HDAC inhibition is achieved via zinc chelation of the carbonyl functional group of the chalcone scaffold. Second, zinc chelation is shown by known zinc-binding groups (ZBGs), and the chalcone scaffold enhances the interaction with the target. In each category, there are subdivisions on the basis of the presence or absence of heterocycles, dual inhibition, and any other modifications. Chalcone compounds with hydroxyl (-OH) and methoxy (-OCH3) substituents have shown therapeutic relevance. Although the inhibition of HDACs by chalcone scaffold metal chelation has been shown, it is comparable to or less effective than known ZBGs, such as hydroxamic acids and benzamides. These findings increase the understanding of the ability of the chalcone scaffold to inhibit HDAC activity and explain its effect on cytotoxicity. Analysis of the influence of substituents offered insight into structural optimization. Further research on structural modifications may reveal improved metal chelation and enhanced cytotoxicity.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-09-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148944177","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}
Leonardo Dos Santos Corrêa Amorim, Natasha Cristina da Rocha, Kauê Francisco Corrêa de Souza E Souza, Vitor Won-Held Rabelo, Izabel Christina Nunes de Palmer Paixão
{"title":"Chalcones as a Platform for the Development of Novel Antiviral Agents: A Review.","authors":"Leonardo Dos Santos Corrêa Amorim, Natasha Cristina da Rocha, Kauê Francisco Corrêa de Souza E Souza, Vitor Won-Held Rabelo, Izabel Christina Nunes de Palmer Paixão","doi":"10.2174/0113895575485097260819095146","DOIUrl":"https://doi.org/10.2174/0113895575485097260819095146","url":null,"abstract":"<p><strong>Introduction: </strong>Viruses pose serious threats to public health, with frequent outbreaks of emerging and reemerging viral pathogens. Given the limitations of current antiviral therapies, the search for new control strategies is essential. In this context, chalcones have attracted great attention due to their structural versatility and a wide range of pharmacological activities, including antiviral effects.</p><p><strong>Methods: </strong>We conducted a literature review examining the antiviral applications of natural and synthetic chalcones validated in experimental assays and reported in articles published up to December 2025 in the PubMed, Web of Science, and Google Scholar databases.</p><p><strong>Results: </strong>Chalcones have shown antiviral activity against more than 15 viral species, including respiratory viruses and arboviruses, human retroviruses, DNA viruses, and the plant pathogen tobacco mosaic virus.</p><p><strong>Discussion: </strong>Structural modifications of the chalcone core influence their mechanisms of action, which involve diverse targets such as viral proteases, kinases, polymerases, structural proteins, as well as host cell pathways. Nevertheless, limited selectivity likely remains a major challenge hindering further development of these compounds.</p><p><strong>Conclusion: </strong>Overall, the structural versatility of chalcones, their broad-spectrum antiviral activity, and their diverse mechanisms of action highlight their strong potential as antiviral agents. Yet, further optimization and in vivo studies are essential to develop more potent and safer chalcone-based drug candidates.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":4.0,"publicationDate":"2026-08-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148906441","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}