Current drug discovery technologies最新文献

{"title":"The Open, Randomized, Positive Control Clinical Trial of Guluronic Acid (G2013) on SARS-CoV-2 Patients.","authors":"Zahra Aghazadeh,&nbsp;Davod Sanaee Delir,&nbsp;Hamid Reza Gholamrezaie,&nbsp;Arezoo Sadoughi,&nbsp;Amir Nezami Asl,&nbsp;Mehran Noori Sanami,&nbsp;Armita Mahdavi Gorabi,&nbsp;Younes Panahi,&nbsp;Mahsa Taeb,&nbsp;Alireza Razavi,&nbsp;Sara Rafia,&nbsp;Zahra Naderiyan,&nbsp;Behrouz Robat-Jazi,&nbsp;Abbas Mirshafiey","doi":"10.2174/1570163820666230418095115","DOIUrl":"10.2174/1570163820666230418095115","url":null,"abstract":"<p><strong>Introduction: </strong>Recently, the coronavirus disease 2019 (COVID-19) infection, with a vast spectrum of clinical and paraclinical symptoms has been a major health concern worldwide. Therapeutical management of COVID-19 includes antiviral and anti-inflammatory drugs. NSAIDs, as the second-line therapy, are often prescribed to relieve the symptoms of COVID-19. The α-L-guluronic acid (G2013) is a non-steroidal patented (PCT/EP2017/067920) agent with immunomodulatory properties. This study investigated the effect of G2013 on the outcome of COVID-19 in moderate to severe patients.</p><p><strong>Methods: </strong>The disease's symptoms were followed up during hospitalization and for 4 weeks postdischarge in G2013 and control groups. Paraclinical indices were tested at the time of admission and discharge. Statistical analysis was performed on clinical and paraclinical parameters and ICU admission and death rate.</p><p><strong>Results: </strong>The primary and secondary outcomes indicated the efficiency of G2013 on COVID-19 patients' management. There were significant differences in the duration of improvement of fever, coughing, fatigue/malaise. Also, a comparison of paraclinical indices at the time of admission and discharge showed significant change in prothrombin, D-dimer, and platelet. As the main findings of this study, G2013 significantly decreased the percentage of ICU admission (control:17 patients, G2013:1 patient) and death (control: 7 cases, G2013:0).</p><p><strong>Conclusion: </strong>These results conclude that G2013 has sufficient potential to be considered for moderate to severe COVID-19 patients, can significantly reduce the clinical and physical complications of this disease, has a positive effect on modulating the coagulopathy process, and aids in saving lives.</p>","PeriodicalId":10858,"journal":{"name":"Current drug discovery technologies","volume":"20 4","pages":"e180423215957"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9831046","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Recent Advances in the Development of Pyrimidine-based CNS Agents.","authors":"Swati Pant,&nbsp;Sumitra Nain","doi":"10.2174/1570163819666221003094402","DOIUrl":"https://doi.org/10.2174/1570163819666221003094402","url":null,"abstract":"<p><strong>Background: </strong>In the past few decades, considerable progress has been made in CNS drug discovery, and various new CNS agents have been developed. Pyrimidine is an important scaffold in the area of medicinal chemistry. Recently, pyrimidine-containing compounds have been successfully designed as potent CNS agents. Substantial research has been carried out on pyrimidine-bearing compounds to treat different disorders of CNS in various animal models.</p><p><strong>Methods: </strong>Utilizing various databases, including Google Scholar, PubMed, Science Direct, and Web of Science, the literature review was conducted. The specifics of significant articles were discussed with an emphasis on the potency of pyrimidines derivatives possessing CNS activity.</p><p><strong>Results: </strong>Recent papers indicating pyrimidine derivatives with CNS activity were incorporated into the manuscript. (46) to (50) papers included different pyrimidine derivatives as 5-HT agonist/antagonists, (62) to (67) as adenosine agonist/antagonist, (70) to (75) as anticonvulsant agents, (80) to (83) as cannabinoid receptor agonists, (102) to (103) as nicotinic and (110) as muscarinic receptor agonists. The remaining papers (113) to (114) represented pyrimidine-based molecular imaging agents.</p><p><strong>Conclusion: </strong>Pyrimidine and its derivatives have been studied in detail to evaluate their efficacy in overcoming multiple central nervous system disorders. The article covers the current updates on pyrimidine-based compounds as potent CNS and molecular imaging agents and will definitely provide a better platform for the development of potent pyrimidine-based CNS drugs in the near future.</p>","PeriodicalId":10858,"journal":{"name":"Current drug discovery technologies","volume":"20 2","pages":"e031022209428"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9833288","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"PROTAC: A Novel Drug Delivery Technology for Targeting Proteins in Cancer Cells.","authors":"Rajni Bala,&nbsp;Rakesh Sindhu,&nbsp;Reecha Madaan,&nbsp;Shantanu","doi":"10.2174/1570163820666221031124612","DOIUrl":"https://doi.org/10.2174/1570163820666221031124612","url":null,"abstract":"<p><p>The treatment measures of malignant carcinomas are most important for human health. In recent years the use of targeted therapy based on small molecule compounds and identical immunoglobulin has been the most frequently used tool to combat cancerous cells. But there are still several limitations in their clinical development and applications, including their ability to bind multiple molecular target sites, both cell surface receptors and intracellular proteins, promoting a greater risk of toxicity. PROTAC is a novel technology that maintains a balance between protein synthesis and degradation and uses molecules instead of conventional enzyme inhibitors, containing two active domains and a linker to destroy unwanted selective protein (like kinase, skeleton protein and regulatory protein). PROTACs are heterobifunctional nano molecules with a size range of about 10 nanometres that eliminate the protein complexes formed by protein-protein interaction through large and flat surfaces generally defined as \"undruggable\" in conventional drug delivery systems, which include around 85% of proteins present in humans, suggesting their wide application in the field of drug development. Such peptide-based PROTACs have successfully shown targets' destruction in cultured cells (e.g., MetAP-2, and FKBP12^F36V, receptors for estrogens and androgen). However, some obstacles prevent this technology from transferring from the laboratory to its actual clinical utility, such as delivery system and bioavailability. The scope of the presented review is to give an overview of novel PROTAC technology with its limitations, advantages, mechanism of action, and development of photocontrolled PROTACs and to summarize its futuristic approach to targeting proteins in cancer cells.</p>","PeriodicalId":10858,"journal":{"name":"Current drug discovery technologies","volume":"20 2","pages":"e311022210504"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9767482","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"One-Step Preparation of Luteolin Nanoemulsion and Evaluation of its Anti-inflammatory Effect in Animal Models.","authors":"Somayyeh Karami-Mohajeri,&nbsp;Narges Hashemi,&nbsp;Mehdi Ranjbar,&nbsp;Mohammad Mohajeri,&nbsp;Fariba Sharififar","doi":"10.2174/1570163820666230327133142","DOIUrl":"https://doi.org/10.2174/1570163820666230327133142","url":null,"abstract":"<p><strong>Background: </strong>Nanoemulsions are promising drug delivery systems for topical application owing to the high transdermal penetration.</p><p><strong>Objective: </strong>Due to the side effects of existing anti-inflammatory drugs, much attention has been paid to natural products such as flavonoids. The aim of this work was to formulate luteolin nanoemulsion (LNE) and to evaluate its anti-inflammatory effect.</p><p><strong>Methods: </strong>LNE was prepared using the low-energy spontaneous emulsion method and characterized by transmission electron microscopy (TEM), Fourier transform infrared (FTIR) spectroscopy and dynamic light scattering (DLS). The anti-inflammatory effect of LNE was assessed in formalin and acetic acid-induced inflammation methods (Whittle test). Treatment with LNE (i.p, 4 consecutive days, 40 mg/kg) was compared with diclofenac 25 mg/kg and normal saline. In the formalin test, data were recorded at 1, 2 and 4 hours after formalin injection and in the Wittle test, the extent of Evans blue leakage in the peritoneal cavity was considered as vascular permeability.</p><p><strong>Results: </strong>Formalin-induced edema decreased in the LNE group, but this reduction was not significant (p > 0.05), however, in Whittle test, both LNE and diclofenac significantly reduced Evans blue leakage compared with the group treated with acetic acid alone (p < 0.05).</p><p><strong>Conclusion: </strong>Our results confirm the anti-inflammatory effect of LNE and give up a new platform for the design and development of bio-based carriers for more successful drug delivery.</p>","PeriodicalId":10858,"journal":{"name":"Current drug discovery technologies","volume":"20 3","pages":"e270323215003"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9768036","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"<i>In silico</i> Study of the Proteins Involved in the Persistence of <i>Brucella</i> spp.","authors":"Parisa Asadollahi,&nbsp;Nourkhoda Sadeghifard,&nbsp;Hossein Kazemian,&nbsp;Iraj Pakzad,&nbsp;Behrooz Sadeghi Kalani","doi":"10.2174/1570163819666220805161821","DOIUrl":"https://doi.org/10.2174/1570163819666220805161821","url":null,"abstract":"<p><strong>Background: </strong>One of the major problems with Brucella infections is its tendency to become chronic and recurrent, providing a hindrance to the management of this infection. It has been proposed that chronicity is greatly affected by a phenomenon called persistence in bacteria. Several mechanisms are involved in bacterial persistence, including the type II toxin-antitoxin system, the SOS and oxidative and stringent responses.</p><p><strong>Methods: </strong>In this in silico study, these persistence mechanisms in Brucella spp. were investigated.</p><p><strong>Results: </strong>The structure and the interactions between modules involved in these systems were designed, and novel peptides that can interfere with some of these important mechanisms were developed.</p><p><strong>Conclusion: </strong>Since peptide-based therapeutics are a new and evolving field due to their ease of production, we hope that peptides developed in this study, as well as the information about the structure and interactions of modules of persistence mechanisms, can further be used to design drugs against Brucella persister cells in the hope of restraining the chronic nature of Brucellosis.</p>","PeriodicalId":10858,"journal":{"name":"Current drug discovery technologies","volume":"20 1","pages":"e050822207324"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9832819","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Herbal Therapies for Weight Gain and Metabolic Abnormalities Induced by Atypical Antipsychotics: A Review Article.","authors":"Hamideh Naghibi,&nbsp;Roshanak Salari,&nbsp;Mahdi Yousefi,&nbsp;Majid Khadem-Rezaiyan,&nbsp;Mohammad Reza Ghanbarzadeh,&nbsp;Mohammad Reza Fayyazi Bordbar","doi":"10.2174/1570163820666230411111343","DOIUrl":"https://doi.org/10.2174/1570163820666230411111343","url":null,"abstract":"<p><p>Psychosis is a state of mind that makes it difficult to determine what is real and what is not. Psychosis can have serious negative effects. Like many psychiatric phenomena, psychosis has a variety of causes, such as schizophrenia, bipolar disorder, and psychotic depression. Antipsychotic medications, psychotherapy, and social support are the most common treatments. Antipsychotic drugs reduce the symptoms of psychosis by changing brain chemistry. Based on the mechanism of action, antipsychotics have two groups, typical and atypical. Most people who take antipsychotics experience side effects. People taking typical antipsychotics tend to have higher rates of extrapyramidal side effects, but some atypical drugs, especially olanzapine, are associated with the risk of significant weight gain, diabetes, and metabolic syndrome, which, in turn, increases the risk of atherosclerotic cardiovascular disease and premature death. Physical exercise, diet regimen, psychoeducation, monotherapy, or switching to an alternative antipsychotic are strategies to correct metabolic aberrates in atypical antipsychotic users. In light of several successful studies on the use of medicinal plants to control metabolic syndrome, this article briefly reviews the studies on some herbal medications for the management of metabolic disorders associated with atypical antipsychotics and discusses probable mechanisms. Therefore, we searched the Cochrane, Scopus, PubMed, and Google Scholar databases for works published before July, 2022, on the effect of herbal medications on antipsychotic-related metabolic abnormalities in animals or humans. We recommend that some herbal medicines may be efficient for regulating the metabolic changes related to atypical antipsychotics due to their multipotential action, and more efforts should be made to make herbal drug treatments more effective. We hope this review will be a reference for research on developing herbal therapeutics for metabolic alterations in antipsychotic customers.</p>","PeriodicalId":10858,"journal":{"name":"Current drug discovery technologies","volume":"20 5","pages":"e110423215660"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10131996","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Biosynthesis of Zinc Oxide Nanoparticles by <i>Lactobacillus</i> spp. and Investigation of their Antimicrobial Effect.","authors":"Saeideh Morovaty Sharifabady,&nbsp;Pegah Shakib,&nbsp;Behin Omidi,&nbsp;Mohammad Reza Zolfaghari","doi":"10.2174/1570163820666230501152951","DOIUrl":"https://doi.org/10.2174/1570163820666230501152951","url":null,"abstract":"<p><strong>Background: </strong>Nanoparticle biology is preferable to other common methods due to its economic efficiency and compatibility with the environment. On the other hand, the prevalence of drug-resistant bacterial strains is expanding and it is necessary to use alternative antibiotic compounds to deal with them. The aim of the present study was the biosynthesis of zinc oxide nanoparticles(ZnO NPs) by Lactobacillus spp. and their antimicrobial effect.</p><p><strong>Methods: </strong>In this study, after the biosynthesis of ZnO NPs by Lactobacillus spp, Characterization of Nanoparticulation Was performed by UV-Vis, XRD, and Scanning Electron Microscopy (SEM). Additionally, Lactobacillus spp. - ZnO NPs were assessed for their antimicrobial properties.</p><p><strong>Results: </strong>UV-visible spectroscopy confirmed the Lactobacillus spp. - ZnO NPs absorbed UV in the region of 300-400 nm. XRD analysis showed the presence of zinc metal in nanoparticles. SEM revealed that Lactobacillus plantarum - ZnO NPs were smaller than the others. Staphylococcus aureus showed the largest non-growth halo diameter against ZnO NPs synthesized by L. plantarum ATCC 8014 (3.7 mm). E. coli had the largest growth halo diameter against ZnO NPs synthesized by L. casei (3 mm) and L. plantarum (2.9 mm). The MIC values of ZnO NPs synthesized by L. plantarum ATCC 8014, L.casei ATCC 39392, L. fermenyum ATCC 9338, L. acidophilus ATCC 4356 were 2,8,8 and 4 μg/mL for Staphylococcus aureus. The MIC values of ZnO NPs synthesized by L. plantarum ATCC 8014, L. casei ATCC 39392, L. fermenyum ATCC 9338, L. acidophilus ATCC 4356 were 2, 4, 4, and 4 μg/ml for E. coli. The lowest MICs were 2 μg/ml for E. coli and S. aureus related to ZnO NPs synthesized by L. plantarum ATCC 8014. MIC and MBC values were equivalent to each other.</p><p><strong>Conclusion: </strong>The results of this research show that ZnO NPs synthesized by L. plantarum ATCC 8014 have more antimicrobial effects than other ZnO NPs used. Therefore, the ZnO NPs made with Lactobacillus plantarum ATCC 8014 have the potential to kill bacteria and can be considered a candidate for antibiotic replacement.</p>","PeriodicalId":10858,"journal":{"name":"Current drug discovery technologies","volume":"20 5","pages":"e010523216388"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10507798","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Acute Toxicity Study of 5, 11-Dihydroindolo [3, 2-ß]carbazole as per OECD Regulatory Guidelines.","authors":"Navyashree V Gowda,&nbsp;Shailesh Bhosale,&nbsp;Anoop Kumar","doi":"10.2174/1570163819666220429095155","DOIUrl":"https://doi.org/10.2174/1570163819666220429095155","url":null,"abstract":"<p><strong>Background: </strong>5,11-Dihydroindolo [3, 2-ß]carbazole is one of the phytoconstituent of the Arisaema genus, which might have various important biological activities. Recently, we have predicted the antiviral potential of this phytoconstituent against the Japanese Encephalitis virus (JEV).</p><p><strong>Methods: </strong>Thus, in the current study, the acute toxicity profile of 5, 11-dihydroindolo [3, 2-ß]carbazole as per OECD regulatory guidelines in female Wistar rats was evaluated.</p><p><strong>Results: </strong>We did not find any adverse effects, mortality, and altered behaviour in animals after administration of 5, 11-dihydroindolo [3, 2-ß] carbazole at a dose of 300 and 2000 mg/Kg. Furthermore, no significant changes in physiological and haematological parameters were observed. The histopathological study of vital organs also showed no significant changes compared to the control.</p><p><strong>Conclusion: </strong>Based on the findings of the current investigation, 5, 11-dihydroindolo [3, 2-ß]carbazole is a safe phytoconstituent of the Arisaema genus, which can be explored for various biological activities.</p>","PeriodicalId":10858,"journal":{"name":"Current drug discovery technologies","volume":"20 1","pages":"e290422204254"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10153895","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A New Bacteriocin from <i>Latilactobacillus sakei</i>: <i>In vitro</i> and <i>In situ</i> Application.","authors":"Camila Ramão Contesa,&nbsp;Nathieli Bastos de Souza,&nbsp;Guilherme Battú Gonçalo,&nbsp;Luciano Almeida,&nbsp;Ana Paula Manera Ziotti,&nbsp;Caroline Costa Moraes","doi":"10.2174/1567201820666221102095749","DOIUrl":"https://doi.org/10.2174/1567201820666221102095749","url":null,"abstract":"<p><strong>Aims and background: </strong>Natural preservatives are a viable alternative to replace chemical preservatives that have potential toxicity and carcinogenic effects.</p><p><strong>Objective: </strong>To prove the effectiveness in increasing the microbiological stability of Minas Frescal cheese with the addition of a bacteriocin obtained from Latilactobacillus sakei as a natural preservative.</p><p><strong>Methods: </strong>A new broad-spectrum bacteriocin was evaluated for its functional activity in vitro and in situ when applied in the formulation of Minas Frescal cheese. A commercial bacteriocin was used as a positive control.</p><p><strong>Results: </strong>The inhibitory action of the bacteriocin studied was confirmed, with a reduction of 42.86% in the count of coagulase-positive Staphylococcus in relation to the negative control, at the end of the 30 days of study. For the group of thermotolerant coliforms, the bacteriocin studied showed greater efficiency than the commercial preservative. In vitro analyzes showed the inhibitory action of bacteriocin, above 87% inhibition against S. aureus, E. coli and Salmonela enteritidis, and approximately 90% against Listeria monocytogenes.</p><p><strong>Conclusion: </strong>It was concluded that the bacteriocin produced by the Latilactobacillus sakei strain has great potential for application in foods such as Minas Frescal cheese.</p>","PeriodicalId":10858,"journal":{"name":"Current drug discovery technologies","volume":"20 2","pages":"e021122210557"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9767485","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Green Chemistry Approach for the Synthesis of Isoxazole Derivatives and Evaluation of their Anti-epileptic Activity.","authors":"Krishna Chandra Panda,&nbsp;Ravi Kumar Venkata Varaha Bera,&nbsp;Biswa Mohan Sahoo,&nbsp;Parijat Swain","doi":"10.2174/1570163820666230215125043","DOIUrl":"https://doi.org/10.2174/1570163820666230215125043","url":null,"abstract":"<p><strong>Background: </strong>Green strategy involves the design, synthesis, processing, and use of chemical substances by eliminating the generation of chemical hazards. This approach focuses on atom economy, use of safer solvents or chemicals, consumption of energy, and decomposition of the chemical substances to non-toxic materials which are eco-friendly.</p><p><strong>Objective: </strong>So, the microwave irradiated heating method is considered a green and sustainable technique for the development of novel heterocyclic scaffold-like isoxazole derivatives via chalcones. Isoxazole derivatives play a vital role due to their diverse pharmacological activities such as antibiotic (Sulfamethoxazole, Cloxacillin, Flucloxacillin, Cycloserine), anti-fungal (Drazoxolon), Antirheumatic (Leflunomide), antidepressant (Isocarboxazid), antineoplastic (Acivicin), anticonvulsant (Zonisamide), antipsychotic (Risperidone) and anti-inflammatory drugs (Valdecoxib), etc. Methods: The isoxazole derivatives were synthesized with the help of microwave irradiation that follows green chemistry protocol.</p><p><strong>Results: </strong>The titled compounds were subjected to antiepileptic evaluation to determine their therapeutic potential.</p><p><strong>Conclusion: </strong>The use of microwave radiation enhances the rate of the reaction which leads to high selectivity with improved product yields in comparison with the traditional heating methods. The tested compounds exhibited promising antiepileptic activity as compared to the standard drug (Phenytoin).</p>","PeriodicalId":10858,"journal":{"name":"Current drug discovery technologies","volume":"20 3","pages":"e150223213697"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9774495","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}