Current topics in medicinal chemistry最新文献

{"title":"A Comprehensive Review on Flavone Scaffolds: Examining their Structural Modifications and Biological Activities.","authors":"Ramalakshmi N, Dibenthiran S, Arunkumar S, Amuthalakshmi S, Indrakumar S, Nalini Cn","doi":"10.2174/0115680266385536250822095825","DOIUrl":"https://doi.org/10.2174/0115680266385536250822095825","url":null,"abstract":"<p><p>Flavones, an important subgroup of flavonoids, demonstrate a wide range of biological activities. A comprehensive review of the literature on the flavone scaffold elucidates its synthetic methodologies and therapeutic potential in various disease states and demonstrates how structural modifications of the flavone moiety result in high-affinity lead candidates for diverse biological targets. The objective of this review is the systematic examination of the alternative synthetic methods of flavones over the traditional method and their medicinal properties, with brief consideration of their structure-activity relationships (SAR). This structural framework presents opportunities for the discovery of novel, improved, efficacious, and well-tolerated biological agents. This review aimed to provide insights that will aid researchers in the systematic design and synthesis of flavone derivatives, potentially leading to the development of novel therapeutic agents.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-10-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145285882","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Viral Vertical Transmission through the Placenta: The Potential of Natural Products as Therapeutic and Prophylactic Antiviral Agents.","authors":"Ana Flavia S Lima, Rayane M Botelho, Marilene B T Fragoso, Miguel L Silva, Jadriane A Xavier, Alexandre U Borbely, Marilia O F Goulart","doi":"10.2174/0115680266366044250901094542","DOIUrl":"https://doi.org/10.2174/0115680266366044250901094542","url":null,"abstract":"<p><p>Pregnant women are among the most vulnerable groups in human populations. The human placenta, consisting of fetal chorionic villi and maternal basal decidua, is a specialized and transient organ crucial for supporting pregnancy and ensuring the well-being of both the mother and the fetus. Although the placenta has a developed, robust defense system, some pathogens can overcome it and cause a fetal infection that may be lethal. This review examines the defense mechanisms in the placenta against viral infections, how microorganisms bypass these defense barriers to cause illness, and the potential use of natural products in treating viral infections during pregnancy. Research on natural products has shown their promise to serve as an alternative to antiviral therapy, particularly for pregnant women.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-09-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145184738","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"FDA-Approved Fluorine-Containing Molecules in 2024: Significance, Synthesis, and Therapeutic Applications.","authors":"Malla Reddy Gannarapu, Ravi Kumar Nagiri, Madhu Desagoni, Ganga Reddy Velma","doi":"10.2174/0115680266388061250917093142","DOIUrl":"https://doi.org/10.2174/0115680266388061250917093142","url":null,"abstract":"<p><p>For the past 75 years, the development pipeline of fluorinated drugs has exemplified the strategic use of fluorine to enhance key pharmacological properties, including bioavailability, metabolic stability, and target affinity. Consequently, fluorine incorporation has become a cornerstone in drug design, inspiring continuous research and development efforts across both academic and industrial sectors. Each year, numerous reviews highlight the ongoing importance of fluorinated drugs and aim to keep the field updated on emerging advancements. This review provides a comprehensive evaluation of the structural and functional benefits of fluorine in medicinal chemistry, presenting an extensive analysis of FDA-approved fluorine-containing drugs from 2015 to 2024. Special attention is paid to the latest approvals from 2024, with a focus on their mechanisms of action and detailed synthetic methodologies.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-09-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145136926","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"An Overview of Novel Indole Scaffolds with Structural Aspects and Receptor Inhibition for Cancer Treatment.","authors":"Neha Sharma, Anurag Chaudhary","doi":"10.2174/0115680266393974250912071544","DOIUrl":"https://doi.org/10.2174/0115680266393974250912071544","url":null,"abstract":"<p><p>Cancer has consistently posed a concern on a worldwide scale. Numerous studies were conducted to establish the best and most efficient treatment for this illness. We attempted to determine the function and mechanism of indole analogs as molecularly targeted anticancer treatment in this review. These indole analogs target various molecules, influencing the development, growth, and spread of tumors. Target anticancer medications function cytostatically and are typically made to accomplish specific goals, in contrast to traditional chemotherapeutics, which act cytotoxically. Small molecules and macromolecules are a novel class of targeted drugs that resulted from this approach. Certain receptor-targeted drugs are superior to macromolecule medicines in terms of improved patient care. Various receptor inhibitors and tyrosine protein kinase receptors that are currently being targeted by anticancer drugs are studied in this review. The different indole analogs target all of these receptors to identify a successful cancer treatment. The Structural Relationship (SAR) between several indole analogs with anticancer action is also highlighted in the present work.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145130356","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Thiazolidine Derivatives: An Up-to-Date Review of Synthesis and Biological Activity.","authors":"Chaimaa Hatim, Abdelghani Boussetta, Marieme Kacem, Mustapha Dib, Khadija Ouchetto, Abderrafia Hafid, Mostafa Khouili, Hajiba Ouchetto","doi":"10.2174/0115680266386939250917053818","DOIUrl":"https://doi.org/10.2174/0115680266386939250917053818","url":null,"abstract":"<p><strong>Introduction: </strong>Over the past decade, thiazolidine derivatives have become promising heterocyclic compounds in medicinal chemistry, and much research work has been devoted to this ring due to their diverse biological activities, therapeutic potential, and heterocyclic ring-like structure. Several studies have shown that certain thiazolidine derivatives exhibit superior activity compared to standard drugs and hold potential for future pharmaceutical applications. This review comprehensively summarizes the key synthetic strategies for thiazolidine derivatives and highlights their biological activities.</p><p><strong>Methods: </strong>The present study is based on the most recent and extensive research on the Thiazolidine structure in the fields of organic synthesis and biological activities from 2015 to 2024, as well as the most widely used methodologies in recent years.</p><p><strong>Results: </strong>The three methods described in this review for the synthesis of thioazolidine derivatives are the most commonly used in recent decades and have given rise to interesting biological activities and the promotion of compounds with chemical and biological significance.</p><p><strong>Discussions: </strong>The synthesis of compounds with a thiazolidine skeleton plays a vital and interesting role in organic chemistry, with methods that are becoming increasingly sophisticated and easy to use, making it possible to obtain derivatives of biological and pharmacological importance, and a basis for future research.</p><p><strong>Conclusion: </strong>The thiazolidine scaffold provides an efficient synthetic route for constructing complex molecular structures with significant biological activities. Their versatile reactivity makes them particularly interesting in organic chemistry, as well as biochemistry and pharmacology.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145130284","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Oroidins: Marine Pyrrole-Imidazole Alkaloids with Emerging Therapeutic Potential.","authors":"Navin Kumar Tailor, Geeta Deswal, Ajmer Singh Grewal, Kumar Guarve","doi":"10.2174/0115680266391437250909024350","DOIUrl":"https://doi.org/10.2174/0115680266391437250909024350","url":null,"abstract":"<p><strong>Introduction/objective: </strong>Oroidins are marine-derived alkaloids known for their structural complexity and a broad range of pharmacological activities. This review aims to explore their emerging role as promising scaffolds in medicinal chemistry, particularly focusing on their unique chemical structure, diverse biological effects, and recent synthetic advancements.</p><p><strong>Methods: </strong>An extensive literature review was conducted to analyze peer-reviewed articles on the isolation, synthesis, structural characterization, and pharmacological evaluation of oroidins and their derivatives. The review highlights significant developments in synthetic strategies, including the incorporation of pyrrole carboxamide units, isotopic labeling approaches, and palladiumcatalyzed reactions.</p><p><strong>Results: </strong>Oroidins exhibit a wide spectrum of biological activities, including antibacterial, antiviral, antimalarial, antiprotozoal, anticancer, anti-inflammatory, neurotropic, and antimuscarinic properties. Their characteristic pyrrole-imidazole core, containing a glycocyamidine moiety and azepinone ring, has been instrumental in targeting key biological pathways such as kinases, NF-κB, and the Raf/MEK-1/MAPK cascade. Structural modifications have led to enhanced potency and specificity of oroidin-based compounds.</p><p><strong>Discussion: </strong>The findings emphasize the potential of oroidins as lead compounds in drug development. Their structural diversity, bioactivity profile, and ability to inhibit critical cellular targets position them as attractive templates for therapeutic design. However, further research is needed to optimize their pharmacokinetic properties and evaluate their clinical relevance.</p><p><strong>Conclusion: </strong>Oroidins represent a valuable class of marine alkaloids with significant therapeutic promise. Advances in synthetic methodologies have expanded their applicability in drug discovery, supporting continued exploration of these compounds for the development of novel therapeutic agents.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-09-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145085411","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Progress in Synthesis and Therapeutic Applications of Mefloquine: A Review.","authors":"Nidhi Yadav, Divyansh Singh, Ram Singh, Yogesh Kumar Tyagi","doi":"10.2174/0115680266389780250828104634","DOIUrl":"https://doi.org/10.2174/0115680266389780250828104634","url":null,"abstract":"<p><p>Mefloquine is a synthetic antimalarial drug known for its effectiveness in the treatment and prevention of malaria. This belongs to the amino alcohol group of compounds. Its structure consists of a quinoline and piperidine ring, along with two chiral centers, which give rise to four distinct stereoisomers. There are various synthetic methods for preparing this compound from starting materials such as p-trifluoromethylaniline, 4-bromoquinoline, and trifluoroacetimidoyl iodide. In recent years, mefloquine has gained attention for its potential therapeutic applications beyond malaria, with research exploring its use in cancer therapy, parasitic infections, neurological disorders, tuberculosis, and COVID-19. This article covers its synthetic approaches, established application as an antimalarial compound, as well as repurposed therapeutic applications.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-09-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145079764","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The Nitrite-Amines Nexus in Nitrosamine Formation: Mechanisms, Mutagenic Implications, Regulations, and Root Causes in Medicines.","authors":"Yunes M M A Alsayadi, Aditya Shiven, Atul Kabra","doi":"10.2174/0115680266379308250827055006","DOIUrl":"https://doi.org/10.2174/0115680266379308250827055006","url":null,"abstract":"<p><strong>Introduction: </strong>Nitrosamines are genotoxic impurities formed from reactions between amines and nitrosating agents, which are commonly found in many consumer products and pharmaceuticals. Their presence poses serious risks due to their established carcinogenic potential, particularly with long-term exposure.</p><p><strong>Methods: </strong>A comprehensive literature review was conducted using PubMed, Scopus, and Web of Science to investigate the mechanisms, sources, analytical detection methods, and regulatory frameworks of nitrosamine formation. Relevant studies and guidelines were analyzed to identify risk patterns and control strategies.</p><p><strong>Results: </strong>Nitrosamines may form during the synthesis of Active Pharmaceutical Ingredients (APIs), due to excipient contamination, or through degradation during storage. Sensitive techniques, such as LC-MS and GC-MS, enable trace-level detection. Regulatory bodies, including the FDA and EMA, have established Acceptable Intake (AI) limits and mandated risk assessments and control measures.</p><p><strong>Discussion: </strong>Nitrosamine formation is influenced by factors, such as pH, heat, moisture, and the interaction of amines with nitrosating agents. The variability in excipient composition and manufacturing processes adds complexity to prevention efforts, underscoring the need for productspecific risk evaluation.</p><p><strong>Conclusion: </strong>Minimizing nitrosamine contamination requires robust risk assessment, sensitive analytical techniques, and strict adherence to evolving regulatory requirements. This review highlights the importance of proactive control throughout the formulation, manufacturing, and storage stages to ensure patient safety and pharmaceutical quality.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-09-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145079876","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development and Exploration of Organic Compounds as Aldose Reductase Inhibitors: An Overview.","authors":"Bhanupriya Bhrigu, Shikha Sharma, Bimal Krishna Banik","doi":"10.2174/0115680266368117250826105101","DOIUrl":"https://doi.org/10.2174/0115680266368117250826105101","url":null,"abstract":"<p><p>Changes in the body's natural glucose levels have been associated with the onset of diabetes mellitus. It is frequently accompanied by a number of long-term consequences, including cardiovascular disease, retinopathy, nephropathy, and cataracts. Aldose reductase (AR), an enzyme belonging to the aldoketo reductase superfamily, plays a crucial role in the polyol pathway of glucose metabolism by converting glucose into sorbitol. Aldose reductase inhibitors (ARIs), a key target for reducing sorbitol flow through the polyol pathway, may be a new target for treating significant diabetic complications. A variety of structural classes of ARIs have been developed. These include: i) derivatives of carboxylic acids (e.g., Epalrestat, Alrestatin, Zopalrestat, Zenarestat, Ponalrestat, Lidorestat, and Tolrestat); ii) derivatives of spirohydantoins and related cyclic amides (e.g., Sorbinil, Minalrestat, and Fidarestat); and iii) phenolic derivatives (e.g., related to Benzopyran- 4-one and Chalcone). The current review article provides concise details of the various chemical classes that aldose reductase inhibitors play in the treatment of diabetic complications. This also describes the advancements made in ARI research and possible applications by obtaining the required data. The process involves thoroughly searching multiple databases-such as PubMed, ScienceDirect, and SciFinder-for citations.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-09-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145014068","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Recent Advances in Antimicrobial Research.","authors":"Ajay Kumar","doi":"10.2174/0115680266435068250902102329","DOIUrl":"https://doi.org/10.2174/0115680266435068250902102329","url":null,"abstract":"","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-09-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145014105","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}