Future medicinal chemistry最新文献

筛选
英文 中文
Correction. 修正。
IF 3.3 4区 医学
Future medicinal chemistry Pub Date : 2026-07-01 Epub Date: 2026-03-04 DOI: 10.1080/17568919.2026.2641873
{"title":"Correction.","authors":"","doi":"10.1080/17568919.2026.2641873","DOIUrl":"10.1080/17568919.2026.2641873","url":null,"abstract":"","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1945"},"PeriodicalIF":3.3,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13336289/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147354411","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis, biological profiling, and computational investigation of 1,2,4-triazole-5-thione-quinoline Schiff base hybrids. 1,2,4-三唑-5-硫酮-喹啉希夫碱杂化物的合成、生物学分析及计算研究。
IF 3.3 4区 医学
Future medicinal chemistry Pub Date : 2026-07-01 Epub Date: 2026-06-12 DOI: 10.1080/17568919.2026.2684452
Ergün Gültekin, Hacer Doğan, Abdurrahman Atalay, Deniz Canbolat Gültekin, Ahmet İsmail Özkan
{"title":"Synthesis, biological profiling, and computational investigation of 1,2,4-triazole-5-thione-quinoline Schiff base hybrids.","authors":"Ergün Gültekin, Hacer Doğan, Abdurrahman Atalay, Deniz Canbolat Gültekin, Ahmet İsmail Özkan","doi":"10.1080/17568919.2026.2684452","DOIUrl":"10.1080/17568919.2026.2684452","url":null,"abstract":"<p><strong>Aims: </strong>To synthesize novel 1,2,4-triazole-5-thione-quinoline Schiff base hybrids and evaluate their urease inhibitory, antimicrobial, antioxidant, and computational properties.</p><p><strong>Materials and methods: </strong>Two series of compounds, <b>7(a-d)</b> and <b>8(a-d)</b>, were synthesized and structurally characterized by Fourier Transform-Infrared (FT-IR), 1 H/13C Nuclear Magnetic Resonance (NMR), mass spectrometry, and elemental analysis. Urease inhibition was determined spectrophotometrically. Antimicrobial activity was assessed by disc diffusion and broth microdilution methods. Antioxidant activity was evaluated using ferric-reducing antioxidant power (FRAP) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) assays. Density functional theory (DFT) and molecular docking studies were also performed.</p><p><strong>Results and conclusions: </strong>Compounds <b>7c</b> and <b>8c</b> showed the strongest urease inhibitory activity, each with an IC<sub>5</sub><sub>0</sub> value of 1.37 mM. 8c displayed the best docking score (-7.6 kcal/mol), while <b>7c</b> showed favorable binding affinity (-6.9 kcal/mol). Antimicrobial screening revealed selective activity mainly against Gram-positive bacteria and fungi, while Gram-negative bacteria were generally resistant. Compound <b>7d</b> displayed the broadest antimicrobial profile, with minimum inhibition concentration (MIC) values of 39.06 µg/mL against Staphylococcus aureus and 19.53 µg/mL against Streptococcus pyogenes. In antioxidant assays, <b>7d</b> and <b>8d</b> showed the highest FRAP values, whereas <b>8c</b> and <b>8a</b> showed the strongest DPPH radical-scavenging activity. DFT results supported the observed structure-activity relationships.</p>","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1871-1886"},"PeriodicalIF":3.3,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13557564/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148224545","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Ultrasound-assisted 1,2,4-triazole Schiff bases: synthesis, characterization, docking, and dual inhibition of urease and α-glucosidase. 超声辅助1,2,4-三唑席夫碱:脲酶和α-葡萄糖苷酶的合成、表征、对接和双重抑制。
IF 3.3 4区 医学
Future medicinal chemistry Pub Date : 2026-07-01 Epub Date: 2026-05-19 DOI: 10.1080/17568919.2026.2675977
Ergün Gültekin
{"title":"Ultrasound-assisted 1,2,4-triazole Schiff bases: synthesis, characterization, docking, and dual inhibition of urease and α-glucosidase.","authors":"Ergün Gültekin","doi":"10.1080/17568919.2026.2675977","DOIUrl":"10.1080/17568919.2026.2675977","url":null,"abstract":"<p><strong>Aim: </strong>This study aimed to design and synthesize novel 3-pentyl-substituted 1,2,4-triazole-5-thione Schiff base derivatives and evaluate their dual inhibitory potential against urease and α-glucosidase enzymes.</p><p><strong>Materials and methods: </strong>The target compounds (<b>6a-e</b>) were synthesized via an ultrasound-assisted condensation method under mild conditions. Structural characterization was performed using Fourier Transform Infrared (FT-IR), <sup>1</sup>H/<sup>13</sup>C nuclear magnetic resonance (NMR), and Liquid chromatography mass spectrometry (LC-MS) analyses. Enzyme inhibitory activities were evaluated using standard spectrophotometric assays, while molecular docking studies were conducted to investigate binding interactions. <i>In silico</i> absorption, distribution, metabolism, and excretion (ADME) properties were predicted using SwissADME.</p><p><strong>Results: </strong>All compounds exhibited measurable inhibitory activity against both enzymes. Among them, compound <b>6c</b> demonstrated the highest potency (urease IC<sub>50</sub> = 14.14 ± 2.61 μg/mL; α-glucosidase IC<sub>50</sub> = 13.14 ± 0.42 μg/mL), showing activity comparable to reference inhibitors. Docking analysis revealed favorable binding interactions, including hydrogen bonding and hydrophobic contacts, particularly for <b>6c</b>. ADME predictions indicated favorable pharmacokinetic profiles for compounds <b>6a-6d</b>.</p><p><strong>Conclusions: </strong>The results highlight the potential of triazole-Schiff base hybrids as dual-enzyme inhibitors, with compound <b>6c</b> identified as a promising lead for further optimization.</p>","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1701-1711"},"PeriodicalIF":3.3,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13557596/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147971740","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Pyran-core small molecules inhibit basal-like triple-negative breast cancer via proteasome activity. 吡喃核小分子通过蛋白酶体活性抑制基底样三阴性乳腺癌。
IF 3.3 4区 医学
Future medicinal chemistry Pub Date : 2026-07-01 Epub Date: 2026-06-11 DOI: 10.1080/17568919.2026.2684487
Khor Poh Yen, Johnson Stanslas, Mock Phooi Yan, Muhamad Afiq Faisal Yahaya, Lam Kok Wai
{"title":"Pyran-core small molecules inhibit basal-like triple-negative breast cancer via proteasome activity.","authors":"Khor Poh Yen, Johnson Stanslas, Mock Phooi Yan, Muhamad Afiq Faisal Yahaya, Lam Kok Wai","doi":"10.1080/17568919.2026.2684487","DOIUrl":"10.1080/17568919.2026.2684487","url":null,"abstract":"<p><p>This study investigates the nonsymmetrical pentanoid derivative <b>5e</b> as a selective anticancer agent against basal-like triple-negative breast cancer (TNBC). The pyran-core derivative <b>5e</b> demonstrated significant selectivity, effectively suppressing the proliferation of basal-like TNBC HCC-1806 cells (IC<sub>50</sub> = 0.59 ± 0.16 µM; selectivity index = 2-6). Mechanistic studies indicated that <b>5e</b> attenuates proteasome degradation activity via the ubiquitin-proteasome pathway. By promoting the accumulation of ubiquitinated oncoproteins, <b>5e</b> induces G2/M cell cycle arrest and triggers both early and late apoptosis in HCC-1806 cells. Molecular docking simulations further revealed that <b>5e</b> forms stable interactions with the β5 subunit binding site of the 20S proteasome.</p>","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1817-1821"},"PeriodicalIF":3.3,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13557591/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148216962","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Hybridization of isatin and benzoxazolinone via a diethyl spacer: a new scaffold for breast cancer drug discovery. 通过二乙基间隔物杂交isatin和苯并恶唑啉酮:乳腺癌药物发现的新支架。
IF 3.3 4区 医学
Future medicinal chemistry Pub Date : 2026-07-01 Epub Date: 2026-06-11 DOI: 10.1080/17568919.2026.2684434
Garima Chauhan, Sahil Kumar, Dharam Pal Pathak, Deepak Kumar, Ravi Rawat, Azhar Iqbal, Pragya Dubey, Satyam Sharma, Kumari Neha
{"title":"Hybridization of isatin and benzoxazolinone via a diethyl spacer: a new scaffold for breast cancer drug discovery.","authors":"Garima Chauhan, Sahil Kumar, Dharam Pal Pathak, Deepak Kumar, Ravi Rawat, Azhar Iqbal, Pragya Dubey, Satyam Sharma, Kumari Neha","doi":"10.1080/17568919.2026.2684434","DOIUrl":"10.1080/17568919.2026.2684434","url":null,"abstract":"<p><strong>Aim: </strong>The present study mainly focused to design and synthesized isatin and benzoxazolinone hybrids via a diethyl linker and evaluate their anti-breast cancer activities.</p><p><strong>Materials and methods: </strong>Five distinct types of isatin-benzoxazolinone derivatives were designed here using the diethyl chain as a linker, and in these molecules, the ketone group of isatin (IST) was treated with urea, thiourea, hydrazine, semicarbazide, and thiosemicarbazide resulting in the formation of corresponding schiff-base derivatives. The binding interactions of all five designed compounds were explored along with the reference ligands axitinib and sorafenib, with the vascular endothelial growth factor receptor-2 (VEGFR-2) (PDB ID: 4AG8) molecular docking and molecular dynamics (MD) simulations. BIT was then synthesized, characterized by IR, LCMS, <sup>1</sup>H NMR, and further anticancer activity assessed against MCF-7 cell line using sorafenib as standard.</p><p><strong>Results: </strong>Molecular docking revealed that compound BIT (hybrid in which ketone group of isatin clubbed with thiosemicarbazide) exhibited a docking score of -10.2 kcal/mol, surpassing the binding affinities of the reference ligands axitinib and sorafenib, highlighting its promising potential.</p><p><strong>Conclusion: </strong>The BIT compound was evaluated, and the results indicated that it exhibited significant inhibitory activity against MCF-7 cells at a concentration of 30 mM.</p>","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1823-1834"},"PeriodicalIF":3.3,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13557559/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148217011","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Design and evaluation of multi-target AGEs/ALEs inhibitors for potential application in skin anti-aging. 多靶点AGEs/ALEs抑制剂在皮肤抗衰老应用的设计与评价。
IF 3.3 4区 医学
Future medicinal chemistry Pub Date : 2026-07-01 Epub Date: 2026-05-28 DOI: 10.1080/17568919.2026.2678790
N André Sasaki, Pascal Sonnet
{"title":"Design and evaluation of multi-target AGEs/ALEs inhibitors for potential application in skin anti-aging.","authors":"N André Sasaki, Pascal Sonnet","doi":"10.1080/17568919.2026.2678790","DOIUrl":"10.1080/17568919.2026.2678790","url":null,"abstract":"<p><p>The main causes of skin aging include both intrinsic and extrinsic factors such as oxidative stress triggered by reactive oxygen species (ROS), modification of collagen and elastin by reactive carbonyl species (RCS), UV exposure, lifestyle habits and environmental pollutants. Skin aging is the most visible manifestation of senescence and is unavoidable. In particular, delaying age-related changes in facial appearance is a key objective for older adults. To address this issue, naturally occurring compounds including vitamin C, vitamin E, coenzyme Q10, resveratrol, niacinamide, carnosine, retinols (vitamin A derivatives), and hyaluronic acid are commonly used in commercially available anti-aging skincare products. These compounds are considered to be ROS and RCS scavengers or powerful humectant. This article describes a new multi-targeted anti-aging compounds for skin applications, composed of two functional moieties: one that neutralizes ROS and the other scavenges RCS. These compounds exhibit potent skin anti-aging properties, as demonstrated by their rapid and efficient scavenging of RCS, an ORAC value more than twice that of Trolox, and strong transition-metal-chelating activity.</p>","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1887-1893"},"PeriodicalIF":3.3,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13557583/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148041743","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Small molecule dual inhibitors of HDAC6/HSP90 as potential anticancer therapeutics: an overview of design rationality and structure activity relationships. HDAC6/HSP90小分子双抑制剂作为潜在的抗癌药物:设计合理性和构效关系综述
IF 3.3 4区 医学
Future medicinal chemistry Pub Date : 2026-07-01 Epub Date: 2026-05-20 DOI: 10.1080/17568919.2026.2675978
Sandipan Dash, Sheik Shehensha, Arghya Kusum Dhar, Dilip Kumar Reddy Kandula, Santosh Kapil Kumar Gorti
{"title":"Small molecule dual inhibitors of HDAC6/HSP90 as potential anticancer therapeutics: an overview of design rationality and structure activity relationships.","authors":"Sandipan Dash, Sheik Shehensha, Arghya Kusum Dhar, Dilip Kumar Reddy Kandula, Santosh Kapil Kumar Gorti","doi":"10.1080/17568919.2026.2675978","DOIUrl":"10.1080/17568919.2026.2675978","url":null,"abstract":"<p><p>The inherent limitations of single-target cancer therapies, including drug resistance, toxicity, and inadequate efficacy against heterogeneous tumors, have catalyzed the strategic shift toward multi-targeted agents. The synergistic interplay between histone deacetylase 6 (HDAC6) and heat shock protein 90 (HSP90), two pivotal nodes in oncogenic signaling, presents a compelling rationale for dual inhibition. HDAC6 epigenetically silences tumor suppressors and regulates cell motility, while HSP90 stabilizes a vast array of oncoproteins. Their concurrent inhibition disrupts this powerful axis, promoting the degradation of oncogenic clients, reversing epigenetic silencing, overcoming drug resistance, and inducing apoptosis. This review comprehensively explores the rationale and recent advancements in the medicinal chemistry of HDAC6/HSP90 dual inhibitors. Through the analysis of diverse chemotypes, including hybrid hydroxamate-based scaffolds, fused heterocyclic systems, and bicyclic hydrophobic core derivatives, critical structure-activity relationship (SAR) principles have been elucidated. The integration of four key pharmacophoric elements is preferred for achieving balanced, nanomolar potency: a hydroxamate zinc-binding group (ZBG), a flexible C6-C8 alkyl linker, an aromatic cap group, and an integrated lipophilic resorcinol-based motif for HSP90 binding. This work underscores the immense potential of HDAC6/HSP90 dual inhibitors as a novel, synergistic, and polypharmacological strategy for cancer therapy, providing a clear roadmap for their rational design and future optimization.</p>","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1769-1781"},"PeriodicalIF":3.3,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13557565/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147981264","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Benzimidazole derived hydrazone Schiff bases as potent cholinesterase inhibitors: synthesis, in vitro and in silico approaches. 苯并咪唑衍生的腙希夫碱作为有效的胆碱酯酶抑制剂:合成,体外和硅方法。
IF 3.3 4区 医学
Future medicinal chemistry Pub Date : 2026-07-01 Epub Date: 2026-06-10 DOI: 10.1080/17568919.2026.2684691
Abdul Shakoor, Ahmed A Elhenawy, Aftab Alam, Imtiaz Ahmad, Munir Ur Rahman, Ajmal Khan, Ferjeni Zouidi, Tahani M Almutairi, Ahmed Al-Harrasi, Momin Khan
{"title":"Benzimidazole derived hydrazone Schiff bases as potent cholinesterase inhibitors: synthesis, <i>in vitro</i> and <i>in silico</i> approaches.","authors":"Abdul Shakoor, Ahmed A Elhenawy, Aftab Alam, Imtiaz Ahmad, Munir Ur Rahman, Ajmal Khan, Ferjeni Zouidi, Tahani M Almutairi, Ahmed Al-Harrasi, Momin Khan","doi":"10.1080/17568919.2026.2684691","DOIUrl":"10.1080/17568919.2026.2684691","url":null,"abstract":"<p><strong>Aims: </strong>The current study aimed to synthesize and evaluate benzimidazole Schiff bases as dual acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE).</p><p><strong>Methods: </strong>Ten benzimidazole Schiff bases were synthesized and characterized by spectroscopic techniques. These compounds were assessed for in vitro AChE and BuChE inhibitory activities. Density functional theory (DFT) analysis was carried out to know the electronic properties, while molecular docking studies were performed to expose protein ligand interactions.</p><p><strong>Results: </strong>In the series, compounds (2c, 2f, 2h, 2a, and 2b) displayed potent inhibition against AChE and BuChE comparable to the standard galantamine. DFT study showed that compounds having higher electrophilicity (ω), lower hardness (η), higher softness (σ), and lower energy gap (ε) increase the inhibitory activity. In addition, electron donating groups at meta position of the benzene improved the potency, while docking studies confirmed favorable binding interactions with the active site of the enzymes.</p><p><strong>Discussion: </strong>These consequences show that both geometric and electronic properties have a vital role in determining the cholinesterase inhibition. These derivatives facilitate multiple interactions within the enzyme active site, supporting its potential as biologically relevant nucleus.</p><p><strong>Conclusion: </strong>The experimental and computational findings provide valuable insights for the optimization and rational design of new therapeutic agents for Alzheimer's disease.</p>","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1853-1869"},"PeriodicalIF":3.3,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13557577/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148210712","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Therapeutic potential of spirocyclopropyl oxindoles: latest developments in drug discovery. 螺环丙基氧吲哚的治疗潜力:药物发现的最新进展。
IF 3.3 4区 医学
Future medicinal chemistry Pub Date : 2026-07-01 Epub Date: 2026-05-27 DOI: 10.1080/17568919.2026.2676782
Sowmya Dastari, Nagula Shankaraiah
{"title":"Therapeutic potential of spirocyclopropyl oxindoles: latest developments in drug discovery.","authors":"Sowmya Dastari, Nagula Shankaraiah","doi":"10.1080/17568919.2026.2676782","DOIUrl":"10.1080/17568919.2026.2676782","url":null,"abstract":"<p><p>In the recent past, spirooxindoles have been evolved as captivating structural architectures for the medicinal chemists, owing to their diverse biological activities. In particular, the development of spirocyclopropyl oxindole heterocycles has gained enormous attention as anti-HIV, anti-cancer and anti-viral agents. The incorporation of a cyclopropyl moiety within the oxindole framework has emerged as a powerful tool in modulating physicochemical and biological properties. This review delineates the medicinal chemistry landscape with a comprehensive overview of recent advances, developments in the design and synthesis of spirocyclopropyl oxindole derivatives and summarizes their biological activities across diverse therapeutic areas. Key insights into the mechanism of action were discoursed. In detail, structure-activity relationships (SARs) have been emphasized on how cyclopropyl incorporation modulates the physicochemical and pharmacological profile relative to conventional oxindole analogues in few cases. An emphasis was placed highlighting the interaction of spirocyclopropyl oxindole derivatives with diverse molecular targets. In addition, current challenges, knowledge gaps, and emerging opportunities for further optimization are discussed, positioning these strained ring systems as a promising and evolving chemical space in the modern medicinal chemistry. Future efforts prioritizing this under explored scaffold would unlock new avenues in the development of novel therapeutics.</p>","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1753-1767"},"PeriodicalIF":3.3,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13557587/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148028906","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Urease inhibitors: current advances, therapeutic potentials, and clinical challenges. 脲酶抑制剂:目前的进展、治疗潜力和临床挑战。
IF 3.3 4区 医学
Future medicinal chemistry Pub Date : 2026-07-01 Epub Date: 2026-06-15 DOI: 10.1080/17568919.2026.2684497
Omer Habis Alzoubi, Almu'atasim Khamees, Mohammad Basil Alzu'bi, Sarah Feras Freihat, Aya Attar, Hanan Abo Sameed, Rawan Alzubi, Amen Ahed Alsamarah, Raghad Yousef Yassin, Khayry Al-Shami, Bahaa Al-Trad, Raed M Al-Zoubi, Mazhar Salim Al Zoubi
{"title":"Urease inhibitors: current advances, therapeutic potentials, and clinical challenges.","authors":"Omer Habis Alzoubi, Almu'atasim Khamees, Mohammad Basil Alzu'bi, Sarah Feras Freihat, Aya Attar, Hanan Abo Sameed, Rawan Alzubi, Amen Ahed Alsamarah, Raghad Yousef Yassin, Khayry Al-Shami, Bahaa Al-Trad, Raed M Al-Zoubi, Mazhar Salim Al Zoubi","doi":"10.1080/17568919.2026.2684497","DOIUrl":"10.1080/17568919.2026.2684497","url":null,"abstract":"<p><p>Urease is a nickel-dependent metalloenzyme that catalyzes urea hydrolysis, generating ammonia and elevating local pH, a process implicated in the pathogenesis of <i>Helicobacter pylori</i>-associated peptic ulcer disease (PUD). To identify effective urease inhibitors, acetohydroxamic acid (AHA) remains the only FDA-approved agent, with clinical use constrained by toxicity. This review synthesizes current evidence on urease inhibition strategies, encompassing metal-based complexes, organic derivatives, natural products, peptide inhibitors, nanotechnology-enabled systems, and emerging gene-based approaches. Several candidates, including copper-based compounds and the natural alkaloid palmatine (PAL), demonstrate potent urease inhibition and favorable effects in preclinical models. However, translation to clinical practice is limited by safety concerns, instability, and a paucity of human trials. Advancing hybrid molecules, optimized delivery platforms, and combination therapies may enhance therapeutic efficacy. Rigorous clinical evaluation remains essential to establish urease inhibition as a viable strategy in urease-mediated diseases.</p>","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1907-1923"},"PeriodicalIF":3.3,"publicationDate":"2026-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13557569/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148250326","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
相关产品
×
本文献相关产品
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:604180095
Book学术官方微信
小红书