Vrushali M. Mahadik, Pradeep M. Mhaldar, Mayuri V. Patil, Nisha A. Nerlekar, Padma B. Dandge, Dattaprasad M. Pore
{"title":"噻唑烷酮-双希夫碱杂合物的多组分合成及其抗菌抗氧化活性评价","authors":"Vrushali M. Mahadik, Pradeep M. Mhaldar, Mayuri V. Patil, Nisha A. Nerlekar, Padma B. Dandge, Dattaprasad M. Pore","doi":"10.1002/slct.202405332","DOIUrl":null,"url":null,"abstract":"<p>Highly efficient one-pot multicomponent synthesis of privileged heterocycle thiazolidinone-bis Schiff base hybrids has been achieved employing sulfamic as an efficient catalyst. A library of its derivatives was introduced in moderate to high yield under mild conditions. The synthesized compounds (5a-5j) were diagnosed by spectral methods such as IR, NMR, and mass spectroscopy and screened for antioxidant and antibacterial activities, including DPPH scavenging activity, ferric-reducing power assay, and minimum inhibitory concentration (MIC). Among these, compound 5e demonstrated the best performance across all assays. Specifically, it exhibited the highest DPPH free radical scavenging activity with an IC50 of 37.40 ± 0.79 µg mL<sup>−1</sup>, the most effective ferric reducing power with an IC50 of 40.56 ± 0.16 µg mL<sup>−1</sup> and had MIC values of > 12.5 µg mL<sup>−1</sup> for Escherichia coli and > 6.25 µg mL<sup>−1</sup> for Bacillus subtilis. These findings indicate the potential of compound 5e as a promising candidate for antioxidant and antimicrobial applications. The mechanism of action of compound 5e and the evaluation of its potentiality for therapeutic use will be explored in the near future.</p>","PeriodicalId":146,"journal":{"name":"ChemistrySelect","volume":"10 17","pages":""},"PeriodicalIF":2.0000,"publicationDate":"2025-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Multicomponent Synthesis of Thiazolidinone -Bis Schiff Base Hybrids and Evaluation of Their Antibacterial and Antioxidant Activity\",\"authors\":\"Vrushali M. Mahadik, Pradeep M. Mhaldar, Mayuri V. Patil, Nisha A. Nerlekar, Padma B. Dandge, Dattaprasad M. Pore\",\"doi\":\"10.1002/slct.202405332\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p>Highly efficient one-pot multicomponent synthesis of privileged heterocycle thiazolidinone-bis Schiff base hybrids has been achieved employing sulfamic as an efficient catalyst. A library of its derivatives was introduced in moderate to high yield under mild conditions. The synthesized compounds (5a-5j) were diagnosed by spectral methods such as IR, NMR, and mass spectroscopy and screened for antioxidant and antibacterial activities, including DPPH scavenging activity, ferric-reducing power assay, and minimum inhibitory concentration (MIC). Among these, compound 5e demonstrated the best performance across all assays. Specifically, it exhibited the highest DPPH free radical scavenging activity with an IC50 of 37.40 ± 0.79 µg mL<sup>−1</sup>, the most effective ferric reducing power with an IC50 of 40.56 ± 0.16 µg mL<sup>−1</sup> and had MIC values of > 12.5 µg mL<sup>−1</sup> for Escherichia coli and > 6.25 µg mL<sup>−1</sup> for Bacillus subtilis. These findings indicate the potential of compound 5e as a promising candidate for antioxidant and antimicrobial applications. The mechanism of action of compound 5e and the evaluation of its potentiality for therapeutic use will be explored in the near future.</p>\",\"PeriodicalId\":146,\"journal\":{\"name\":\"ChemistrySelect\",\"volume\":\"10 17\",\"pages\":\"\"},\"PeriodicalIF\":2.0000,\"publicationDate\":\"2025-04-26\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"ChemistrySelect\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://onlinelibrary.wiley.com/doi/10.1002/slct.202405332\",\"RegionNum\":4,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, MULTIDISCIPLINARY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"ChemistrySelect","FirstCategoryId":"92","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1002/slct.202405332","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
引用次数: 0
摘要
以氨基磺酸为催化剂,实现了特权杂环噻唑烷酮-双希夫碱杂化物的高效一锅多组分合成。介绍了在温和条件下中高产量的衍生物文库。合成的化合物(5a-5j)通过IR, NMR和质谱等光谱方法进行诊断,并筛选抗氧化和抗菌活性,包括DPPH清除活性,铁还原能力测定和最小抑制浓度(MIC)。其中,化合物5e在所有试验中表现出最好的性能。其中,DPPH自由基清除能力最强,IC50为37.40±0.79µg mL - 1;铁还原能力最强,IC50为40.56±0.16µg mL - 1, MIC值为>;12.5µg mL−1大肠杆菌和>;枯草芽孢杆菌6.25µg mL−1。这些发现表明化合物5e在抗氧化和抗菌方面具有潜在的应用前景。化合物5e的作用机制及其治疗潜力的评价将在不久的将来进行探索。
Multicomponent Synthesis of Thiazolidinone -Bis Schiff Base Hybrids and Evaluation of Their Antibacterial and Antioxidant Activity
Highly efficient one-pot multicomponent synthesis of privileged heterocycle thiazolidinone-bis Schiff base hybrids has been achieved employing sulfamic as an efficient catalyst. A library of its derivatives was introduced in moderate to high yield under mild conditions. The synthesized compounds (5a-5j) were diagnosed by spectral methods such as IR, NMR, and mass spectroscopy and screened for antioxidant and antibacterial activities, including DPPH scavenging activity, ferric-reducing power assay, and minimum inhibitory concentration (MIC). Among these, compound 5e demonstrated the best performance across all assays. Specifically, it exhibited the highest DPPH free radical scavenging activity with an IC50 of 37.40 ± 0.79 µg mL−1, the most effective ferric reducing power with an IC50 of 40.56 ± 0.16 µg mL−1 and had MIC values of > 12.5 µg mL−1 for Escherichia coli and > 6.25 µg mL−1 for Bacillus subtilis. These findings indicate the potential of compound 5e as a promising candidate for antioxidant and antimicrobial applications. The mechanism of action of compound 5e and the evaluation of its potentiality for therapeutic use will be explored in the near future.
期刊介绍:
ChemistrySelect is the latest journal from ChemPubSoc Europe and Wiley-VCH. It offers researchers a quality society-owned journal in which to publish their work in all areas of chemistry. Manuscripts are evaluated by active researchers to ensure they add meaningfully to the scientific literature, and those accepted are processed quickly to ensure rapid online publication.