Current topics in medicinal chemistry最新文献

{"title":"Copper-Redox Cycling by Flavonoid Alpinetin Leads to ROS-Mediated DNA Damage and Apoptosis: A Mechanism for Cancer Chemoprevention.","authors":"Mohd Farhan, Mohamed El Oirdi, Aamir Ahmad","doi":"10.2174/0115680266433839260131175726","DOIUrl":"https://doi.org/10.2174/0115680266433839260131175726","url":null,"abstract":"<p><p>Introduction / Objective: Polyphenols, present in fruits and vegetables and recognized for their anticancer properties, are generally known for their antioxidant abilities; however, they may exhibit prooxidant behavior in the presence of copper ions.</p><p><strong>Methods: </strong>This study demonstrates that the flavonoid alpinetin inhibits cell growth in the breast cancer cell lines MDA-MB-231 and MCF-7, as evaluated by MTT assay, and induces apoptosislike cell death, as evaluated by Histone/DNA ELISA.</p><p><strong>Results: </strong>We found the effect to be inhibited by neocuproine, a copper chelator, and by the scavengers of reactive oxygen species (ROS). The inhibitory effect suggests that intracellular copper interacts with alpinetin in cancer cells, leading to DNA damage through the generation of ROS. Additionally, a non-tumorigenic epithelial cell line (MCF-10A) grown in copper-supplemented media exhibits increased sensitivity to growth inhibition by alpinetin, as evidenced by a decrease in cell proliferation. Furthermore, copper supplementation enhances copper transporter CTR1's expression in MCF-10A cells, whereas adding alpinetin to the media reduces this expression.</p><p><strong>Discussion: </strong>The findings provide additional support for the notion that a crucial anticancer mechanism of plant polyphenols involves the mobilization of intracellular copper and the generation of ROS, ultimately leading to the apoptosis of cancer cells.</p><p><strong>Conclusion: </strong>These findings demonstrate that alpinetin exerts its anticancer effects through intracellular copper mobilization and ROS generation, ultimately leading to apoptosis in breast cancer cells.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-05-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147835026","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":"Precision Oncology: Emerging Molecular Methods for Drug Target Discovery.","authors":"Dharmendra Kumar Yadav, Desh Deepak Singh, Dongyun Shin","doi":"10.2174/0115680266391057250929110130","DOIUrl":"https://doi.org/10.2174/0115680266391057250929110130","url":null,"abstract":"<p><p>Molecular-targeted cancer therapies aim to block specific molecules essential for tumour growth and survival, resulting in enhanced efficacy and reduced side effects. This review explores various strategies, including angiogenesis inhibition, where tumour expansion is curtailed by disrupting new blood vessel formation. Targeting microtubules affects mitotic spindle formation, which is essential for cell division, thereby hindering the rapid division of cancer cells. The modulation of signal transduction pathways, particularly involving tyrosine kinases and Ras proteins, is pivotal for altering proliferative and survival signals. Metabolic transformations, nucleotide biosynthesis, and cell cycle regulation are also critical targets, given their roles in tumour growth and replication. Additionally, targeting transcription factors like NF-κB and AP-1, alongside growth factors and tumour suppressor genes, such as p53, represents another layer of therapeutic intervention. The review emphasises the significance of apoptosis induction and the inhibition of chemokines, metastasis, and various enzymes like COX-2 and LOX in the comprehensive management of cancer. This perspective focuses on the conceptual framework that has guided the search for innovative anticancer medicines.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-05-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147834949","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":"Antileishmanial Evaluation and Mechanism of Action of Benzothiazole Derivatives with Aromatic/Heteroaromatic Hydrazone Moiety.","authors":"Luciana M R Antinarelli, Alessandra Campbell Pinheiro, Victor Facchinetti, Thatyana R A Vasconcelos, Ari Sérgio de Oliveira Lemos, Adolfo Firmino da Silva Neto, Elaine Soares Coimbra, Marcus Vinícius Nora De Souza","doi":"10.2174/0115680266405459251127053423","DOIUrl":"https://doi.org/10.2174/0115680266405459251127053423","url":null,"abstract":"<p><strong>Introduction: </strong>Treatment of leishmaniasis is limited to a few drugs, with serious side effects and contraindications. Thus, the need for alternatives to treat this neglected infectious disease is undeniable.</p><p><strong>Methods: </strong>In this work, a series of benzothiazole derivatives was synthesized, and their in vitro effects against promastigotes and intracellular amastigotes of Leishmania spp. and their macrophage toxicity were evaluated. Peritoneal macrophages were successful obtained from BALB/c mice were used for intracellular amastigotes of Leishmania spp. assays and to assess their toxicity on mammalian cells. In vitro studies on the mechanism of action and drug combination assays were also performed.</p><p><strong>Results: </strong>Compound 2a exhibited remarkable activity against L. amazonensis and L. infantum, with IC50 values below 5 μM against amastigote forms (3.96 μM and 4.0 μM, respectively), surpassing the reference drug miltefosine, and had no cytotoxic effect on macrophages (CC50 > 150 μM).</p><p><strong>Discussion: </strong>The antileishmanial effect of compound 2a was associated with hyperpolarization of the mitochondrial membrane potential, increased ROS levels, and the formation of lipid bodies in treated promastigote forms of L. amazonensis, indicating mitochondrial dysfunction and oxidative stress. No disruption of the promastigotes' plasma membrane was observed after treatment with this compound, ruling out necrotic cell death. Interactions between compound 2a and miltefosine exhibited a better effect at the lowest concentration of compound 2a (combination 1:4) in both promastigote and amastigote forms of L. amazonensis. In silico analysis showed promising physicochemical properties for compound 2a.</p><p><strong>Conclusion: </strong>Compound 2a displays strong antileishmanial activity against L. amazonensis and L. infantum, demonstrating a broad ability to inhibit the growth of Leishmania species associated with cutaneous and visceral manifestations.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-05-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147835031","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":"Protective Effect of Thymol-loaded Chitosan Nanoparticles against Bile Duct Ligation-induced Liver Fibrosis in Rats.","authors":"Teba Abdelrahman Kamel, Ahmed Abdel Aziz Baiomy, Sarah Ali Qutb, Ayman Saber Mohamed","doi":"10.2174/0115680266391085251022030252","DOIUrl":"https://doi.org/10.2174/0115680266391085251022030252","url":null,"abstract":"<p><strong>Introduction: </strong>Liver fibrosis is a critical disorder associated with elevated morbidity and mortality rates globally, leading to many organ dysfunctions. Thymol is a phenolic aromatic chemical extracted from thyme oil. It possesses biochemical, oxidative, anti-inflammatory, and anticancer properties. This results in its widespread applications across various domains, including cosmetics, medicine, and pharmacology. This study aims to assess the efficiency of thymol-loaded chitosan nanoparticles (CS-thymol NPs) in the bile duct ligation (BDL) model of liver fibrosis.</p><p><strong>Methods: </strong>Thirty male Wister rats were divided into five groups: Sham, BLD, and cholestasis rats treated with chitosan NPs (60 mg/kg body weight, orally), thymol (30 mg/kg body weight, orally), and CS-thymol NPs (60 mg/kg body weight, orally).</p><p><strong>Results: </strong>The administration of CS-thymol NPs markedly enhanced liver function, evidenced by reduced hepatic enzyme activity and elevated albumin level. Furthermore, CS-thymol NPs induced an elevation in glutathione and reduced catalase levels, and along with the reduction in malondialdehyde and nitric oxide production. Furthermore, CS-thymol NPs therapy diminished DNA damage in cholestatic rats and partially restored the normal architecture of hepatic tissues in these subjects. Immunohistochemistry analysis revealed a significant reduction in inflammation and apoptosis by decreasing levels of TNF-α and caspase-3 expression.</p><p><strong>Discussion: </strong>The anticholestatic mechanisms of thymol may depend on its anti-inflammatory activity through the inhibition of TNF-α release, its antioxidative properties by decreasing MDA and NO levels while enhancing CAT and GSH, and its anti-apoptotic effects, likely associated with the down-regulation of activated caspase-3 and DNA damage.</p><p><strong>Conclusion: </strong>The incorporation of thymol into chitosan NPs boosts its antioxidant, antiinflammatory, and anti-apoptotic properties, thereby improving liver function and structure of cholestatic rats.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-05-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147835008","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 Role of Glutathione Insufficiency in Immune Dysfunction and Increased Susceptibility to SARS-CoV-2 Infections in Type 2 Diabetes.","authors":"Vivian Yu, Vivian Zhong, Eashan Sharma, Kevin Babakhan Vartanian, Mohammad J Nasiri, Vishwanath Venketaraman","doi":"10.2174/0115680266395033251019091517","DOIUrl":"https://doi.org/10.2174/0115680266395033251019091517","url":null,"abstract":"<p><p>Glutathione (GSH), a critical antioxidant, plays an essential role in immune function and cellular health. In Type 2 Diabetes Mellitus (T2DM), GSH deficiency exacerbates oxidative stress, impairs immune responses, and increases susceptibility to viral infections, including COVID-19. Chronic hyperglycemia, inflammation, and oxidative damage characteristic of T2DM create a pathological environment that heightens the risk of severe outcomes. This review explores mechanisms linking GSH insufficiency to worsened viral infections, immune dysfunction, and complications such as Acute Respiratory Distress Syndrome (ARDS) and thrombosis. We focus on GSH's role in SARS-CoV-2 replication and how its deficiency impairs immune defenses, increasing vulnerability in T2DM patients. Potential therapeutic strategies to restore GSH levels, including Nacetylcysteine (NAC) supplementation and liposomal GSH, are discussed. Addressing GSH deficiency may enhance resilience to infections and reduce disease severity in T2DM. By unraveling molecular connections between GSH insufficiency, immune dysfunction, and viral pathogenesis, novel therapies may improve outcomes and mitigate infection severity.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-05-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147835003","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":"Discovery of Novel Quinazoline Thiazole Uredio Analogs as Dual Inhibitors of GSK-3β and CK-1δ as Anti-Alzheimer's Agents: Catching Two Fish with One Net.","authors":"Dileep Kumar, Vinayak Walhekar, Mangala Shenoy Kasaragod, Suvarna Kini","doi":"10.2174/0115680266378266251017045841","DOIUrl":"https://doi.org/10.2174/0115680266378266251017045841","url":null,"abstract":"<p><strong>Introduction: </strong>AD is a widespread and debilitating neurodegenerative disorder, and existing treatments have demonstrated limited efficacy, emphasizing the need for novel therapeutic strategies. This study focused on the design of drug-like molecules with enhanced efficacy and minimized side effects through the application of structure-based scaffold hopping and molecular hybridization strategies.</p><p><strong>Methods: </strong>Molecular docking was carried out on the Glide module, Molecular dynamics simulation of 500 ns was executed employing Desmond, and ADMET prediction was achieved by the QikProp modules of Schrodinger.</p><p><strong>Results: </strong>Through molecular docking studies targeting the GSK-3β and CK-1δ enzymes, the compounds VDK12 and VDK14 were identified as promising inhibitors, showing favorable interactions within the active sites of these proteins, with docking energies of -9.9 kcal/mol and -10.1 kcal/mol, respectively. Molecular dynamics simulations further revealed that the VDK12 and VDK14 complexes exhibited stable interactions within the active sites of GSK-3β and CK-1δ throughout a 500 ns simulation. Additionally, in silico ADMET analysis demonstrated that VDK1 exhibited an excellent human oral absorption rate of 91.349%, outperforming other compounds in the series.</p><p><strong>Discussion: </strong>Molecules as dual inhibitors were designed successfully by the application of scaffold hopping and molecular hybridization. Designed molecules demonstrated excellent molecular docking and dynamics simulation results with an appropriate ADMET profile.</p><p><strong>Conclusion: </strong>These findings strongly suggest the potential of VDK12 and VDK14 as dual inhibitors of GSK-3β and CK-1δ, offering a promising foundation for the development of new lead compounds for AD treatment.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147835000","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":"Natural Products-Inspired Drug Discovery Using Computer-Aided Drug Design Techniques.","authors":"Harish C Upadhyay","doi":"10.2174/0115680266499782260427045530","DOIUrl":"https://doi.org/10.2174/0115680266499782260427045530","url":null,"abstract":"","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147834954","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":"Pharmacological Study of Imidazolium and Pyridinium Salts with Antifungal Activity against Chromoblastomycosis Agents.","authors":"Leonardo Girardi Ransan, Igor Luiz Gonçalvez Pereira, Michele Oliveira Hütten, Ianka Jacondino Nunes, Daiane Heidrich, Régis Adriel Zanette, Henri Stephan Schrekker, Jenifer Saffi, Valeriano Antonio Corbelini, Maria Lúcia Scroferneker","doi":"10.2174/0115680266407632251202155630","DOIUrl":"https://doi.org/10.2174/0115680266407632251202155630","url":null,"abstract":"<p><strong>Background: </strong>Chromoblastomycosis (CBM) is a subcutaneous fungal infection caused by melanized fungi, predominantly in tropical and subtropical climates. CBM-causing fungal strains are becoming resistant to antifungal drugs, leading to prolonged treatments and low cure rates. Therefore, the development of new antifungals to combat this disease is a priority.</p><p><strong>Objectives: </strong>This study explored imidazolium salts (IS) and a pyridinium salt (PS) as candidate drugs for the treatment of CBM. Their pharmacological properties were investigated as possible therapeutic alternatives to itraconazole (ITZ).</p><p><strong>Methods: </strong>In silico analyses were performed using Lipinski's rule of five (Ro5). Seventy-eight isolates of CBM-causing fungi were tested following the CLSI M38-A2 protocol to determine minimal inhibitory concentrations (MIC) and minimal fungicidal concentrations (MFC). Fourier transform infrared spectroscopy (FTIR) was applied to compare the compound with the lowest MFC against standard antifungals. Cytotoxicity was evaluated using the neutral red (NR) and methyl thiazole tetrazolium (MTT) assays, and genotoxicity was assessed by the alkaline comet assay. In vivo toxicity was tested in Drosophila melanogaster.</p><p><strong>Results: </strong>The in silico analysis indicated probable antifungal activity with low toxicity in humans. The compounds exhibited lower MIC and MFC values than ITZ, with C16PyrCl showing the lowest MFC (0.474 μg/mL). FTIR analysis confirmed distinct alterations in fungal biomass metabolism compared with standard antifungals. Cytotoxicity and genotoxicity assays revealed elevated toxicity of IS toward mammalian cells; however, no toxicity was observed in D. melanogaster.</p><p><strong>Discussion: </strong>The tested compounds showed strong activity against CBM agents, although they also presented cytotoxic and genotoxic effects on animal cells. Metabolic alterations between the chosen PS and existing antifungals were successfully described using FTIR spectroscopy.</p><p><strong>Conclusions: </strong>The compounds demonstrated potent fungicidal activity against CBM-causing fungi, highlighting their potential as antifungal candidates. Further in vivo studies are required to optimize their safety and therapeutic applicability.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147834974","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 Functional Chelators for PET and SPECT Imaging Probes.","authors":"Juno Van Valkenburgh, Asneh Singh, Quan Chen, Austin Z Chen, Chuansheng Zheng, Kai Chen","doi":"10.2174/0115680266441414260109060017","DOIUrl":"https://doi.org/10.2174/0115680266441414260109060017","url":null,"abstract":"<p><p>Positron Emission Tomography (PET) and Single-Photon Emission Computed Tomography (SPECT) are two of the most frequently employed molecular imaging modalities for interrogating biological processes in living systems. A significant number of recently developed probes are based on radiometals. Radiometal-based compounds use a chelator for radionuclide complexation and linkage to a targeting molecule. In practice, selecting the \"right\" chelator has consequences that extend well beyond simple coordination chemistry, influencing labeling conditions, probe stability, in vivo behavior, and ultimately diagnostic performance. As a result, both acyclic and cyclic chelators have been explored extensively. Acyclic chelators, such as DTPA, HBED, DFO, and HYNIC, are attractive because they can be labeled rapidly under mild conditions, but their in vivo stability is not always sufficient for clinical use. In contrast, macrocyclic chelators, such as DOTA, NOTA, TETA, and sarcophagines, are more kinetically inert, though they often demand higher temperatures or more stringent labeling parameters. Over the past decades, several innovations have been made, such as [18F]AlF-NOTA chemistry, optimized DFO derivatives for 89Zr, and copper-specific sarcophagines. This emerging landscape of PET and SPECT radiotracers has broadened the range of applications from neuroendocrine tumors to FAPI-based probes and to theranostic strategies. The refinement and development of bifunctional chelators that allow radiometals to be bound to peptides, antibodies, and nanoparticles without loss of biological activity is opening up new avenues. The field is working toward more kit-based, user-friendly chelators that are applicable to a broad range of radionuclides. In this review, we summarize recent progress in chelator design and show how it is shaping the future of molecular imaging and targeted radionuclide therapy.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147834981","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":"Combining Thiophene-Triazole Hybrids with Bothropic Antivenom to Enhance Its Inhibitory Effect Against the Coagulant Activity of Bothrops Jararaca, B. Neuwiedi, and B. Jararacussu Snake Venoms.","authors":"Brenda Bairral de Oliveira, Eladio Flores Sanchez, Danielle Pagliaminuto Portella, Vitor Francisco Ferreira, Fernando de Carvalho da Silva, Daniel Tadeu Gomes Gonzaga, Andre Lopes Fuly","doi":"10.2174/0115680266460346260318041601","DOIUrl":"https://doi.org/10.2174/0115680266460346260318041601","url":null,"abstract":"<p><strong>Introduction: </strong>Snakebite envenomation causes approximately 5 million incidents, 130,000 deaths, and 400,000 amputations annually worldwide. Thus, the objective of this work was to assess the ability of 16 thiophene-triazole hybrid compounds (6a-6h and 7a-7h) to inhibit the coagulant activity of Bothrops jararaca, B. neuwiedi, and B. jararacussu venoms in combination with commercial antibothropic antivenom.</p><p><strong>Method: </strong>In the experimental prevention protocol, human plasma or commercial fibrinogen was incubated for 60 seconds at 37°C with the study compounds, with or without antivenom, followed by the addition of snake venoms. In the treatment protocol, each venom was incubated with plasma or fibrinogens for 60 seconds at 37°C, and then the study compounds, with or without antivenom, were added to the medium. Clotting was monitored using a digital coagulometer.</p><p><strong>Results: </strong>The study compounds inhibited the coagulation of plasma and fibrinogen caused by B. neuwiedi venom under both protocols, but they did not inhibit B. jararacussu venom under the treatment protocol. Overall, the coagulation inhibition was more effective when the study compounds were mixed with antivenom, and some compounds achieved complete prevention of venom- induced coagulation.</p><p><strong>Discussion: </strong>A combination of compounds with antivenom enhanced efficacy in preventing the coagulant activity of Bothrops venoms.</p><p><strong>Conclusion: </strong>A drug cocktail comprising the most active compounds mixed with antivenom may be a promising strategy to improve the treatment of envenomation by these snake species.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147722018","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}