3-氨基-1,2,4-三唑-5-硫酸盐新型席夫碱的设计、合成、表征及作为抗菌药物的生物学评价

{"title":"3-氨基-1,2,4-三唑-5-硫酸盐新型席夫碱的设计、合成、表征及作为抗菌药物的生物学评价","authors":"","doi":"10.25163/angiotherapy.717333","DOIUrl":null,"url":null,"abstract":"Schiff bases (T1-T10) were prepared from the reaction of various benzaldehyde derivatives with 3-amino-1,2,4-triazole-5-thiol in the presence of Morpholine, and all the prepared compounds were characterized using UV, FIR spectroscopy, in addition to GC-Mass, 1H-NMR for some combinations and measuring their melting points. The obtained results confirmed the validity of the proposed structures of the prepared compounds. The biological activity of all prepared compounds (T1-T10) was tested against four types of Gram-positive and Gram-negative bacteria. The study showed that the compound T8 inhibited Staphylococcus aureus with an IC50 of 22 µg/mL, followed by T1, T10, T2, and T3 with IC50 values of 25, 26, 33, and 33 µg/mL, respectively. In addition, T3, T10, T2, T1, and T4 had an inhibitory effect on Pseudomonas aeruginosa with IC50 values of 22, 28, 39, 44, and 50 µg/mL, respectively. T4, T2, and T5 inhibited Streptococcus mutans with IC50 values of 28, 32, and 38 µg/mL, respectively. Interestingly, T6 had the strongest inhibitory effect on Klebsiella pneumoniae with an IC50 of 15 µg/mL. The results of this study suggest that T8, T3, T4, and T6 may be potential new antibiotics for the treatment of Staphylococcus aureus, Pseudomonas aeruginosa, Streptococcus mutans, and Klebsiella pneumoniae. However, further studies are needed to confirm these findings and to evaluate the safety and efficacy of these compounds in humans.","PeriodicalId":154960,"journal":{"name":"Journal of Angiotherapy","volume":"44 1","pages":"0"},"PeriodicalIF":0.0000,"publicationDate":"2023-07-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Design, Synthesis, And Characterization Of New Schiff Bases For 3-Amino-1,2,4-Triazole-5-Thiolate Salt, Bearing Morpholine Ring And Biological Evaluation As Antibacterial Agents\",\"authors\":\"\",\"doi\":\"10.25163/angiotherapy.717333\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Schiff bases (T1-T10) were prepared from the reaction of various benzaldehyde derivatives with 3-amino-1,2,4-triazole-5-thiol in the presence of Morpholine, and all the prepared compounds were characterized using UV, FIR spectroscopy, in addition to GC-Mass, 1H-NMR for some combinations and measuring their melting points. The obtained results confirmed the validity of the proposed structures of the prepared compounds. The biological activity of all prepared compounds (T1-T10) was tested against four types of Gram-positive and Gram-negative bacteria. The study showed that the compound T8 inhibited Staphylococcus aureus with an IC50 of 22 µg/mL, followed by T1, T10, T2, and T3 with IC50 values of 25, 26, 33, and 33 µg/mL, respectively. In addition, T3, T10, T2, T1, and T4 had an inhibitory effect on Pseudomonas aeruginosa with IC50 values of 22, 28, 39, 44, and 50 µg/mL, respectively. T4, T2, and T5 inhibited Streptococcus mutans with IC50 values of 28, 32, and 38 µg/mL, respectively. Interestingly, T6 had the strongest inhibitory effect on Klebsiella pneumoniae with an IC50 of 15 µg/mL. The results of this study suggest that T8, T3, T4, and T6 may be potential new antibiotics for the treatment of Staphylococcus aureus, Pseudomonas aeruginosa, Streptococcus mutans, and Klebsiella pneumoniae. However, further studies are needed to confirm these findings and to evaluate the safety and efficacy of these compounds in humans.\",\"PeriodicalId\":154960,\"journal\":{\"name\":\"Journal of Angiotherapy\",\"volume\":\"44 1\",\"pages\":\"0\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2023-07-29\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Angiotherapy\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.25163/angiotherapy.717333\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Angiotherapy","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.25163/angiotherapy.717333","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0

摘要

以不同的苯甲醛衍生物为原料,在啉存在下与3-氨基-1,2,4-三唑-5-硫醇反应制备了希夫碱(T1-T10),并利用紫外光谱、FIR光谱、GC-Mass、1H-NMR对所制备的化合物进行了表征,并测定了其熔点。所得结果证实了所制备化合物结构的有效性。所有化合物(T1-T10)对4种革兰氏阳性菌和革兰氏阴性菌的生物活性进行了测试。研究表明,化合物T8对金黄色葡萄球菌的抑制作用IC50值为22µg/mL,其次是T1、T10、T2和T3, IC50值分别为25、26、33和33µg/mL。T3、T10、T2、T1、T4对铜绿假单胞菌均有抑制作用,IC50值分别为22、28、39、44、50µg/mL。T4、T2、T5对变形链球菌的抑制作用IC50值分别为28、32、38µg/mL。有趣的是,T6对肺炎克雷伯菌的抑制作用最强,IC50为15µg/mL。本研究结果提示,T8、T3、T4和T6可能是治疗金黄色葡萄球菌、铜绿假单胞菌、变形链球菌和肺炎克雷伯菌的潜在新型抗生素。然而,需要进一步的研究来证实这些发现,并评估这些化合物在人体中的安全性和有效性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
查看原文
分享 分享
微信好友 朋友圈 QQ好友 复制链接
本刊更多论文
Design, Synthesis, And Characterization Of New Schiff Bases For 3-Amino-1,2,4-Triazole-5-Thiolate Salt, Bearing Morpholine Ring And Biological Evaluation As Antibacterial Agents
Schiff bases (T1-T10) were prepared from the reaction of various benzaldehyde derivatives with 3-amino-1,2,4-triazole-5-thiol in the presence of Morpholine, and all the prepared compounds were characterized using UV, FIR spectroscopy, in addition to GC-Mass, 1H-NMR for some combinations and measuring their melting points. The obtained results confirmed the validity of the proposed structures of the prepared compounds. The biological activity of all prepared compounds (T1-T10) was tested against four types of Gram-positive and Gram-negative bacteria. The study showed that the compound T8 inhibited Staphylococcus aureus with an IC50 of 22 µg/mL, followed by T1, T10, T2, and T3 with IC50 values of 25, 26, 33, and 33 µg/mL, respectively. In addition, T3, T10, T2, T1, and T4 had an inhibitory effect on Pseudomonas aeruginosa with IC50 values of 22, 28, 39, 44, and 50 µg/mL, respectively. T4, T2, and T5 inhibited Streptococcus mutans with IC50 values of 28, 32, and 38 µg/mL, respectively. Interestingly, T6 had the strongest inhibitory effect on Klebsiella pneumoniae with an IC50 of 15 µg/mL. The results of this study suggest that T8, T3, T4, and T6 may be potential new antibiotics for the treatment of Staphylococcus aureus, Pseudomonas aeruginosa, Streptococcus mutans, and Klebsiella pneumoniae. However, further studies are needed to confirm these findings and to evaluate the safety and efficacy of these compounds in humans.
求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
自引率
0.00%
发文量
0
期刊最新文献
Synthesis And In-Silico Anti-Cancer Potential of N-Aryl-Keto-Nitrone As A Spin Adducts Gut-Brain Connection; IBS linked to Anxiety, Quality of Life, and Academic Performance in Undergraduate Students Two Forms of C-Reactive Protein and Their Implication for Atherogenesis: Focus on Monomeric Form Therapeutic Effects of Esomeprazole, Curcumin, Chitosan, and Curcumin-Chitosan Mixture on Ethanol-Induced Gastric Ulcer in Female Rats Significance of Serum Biomarkers in Early Diagnosis of Hepatocellular Carcinoma in Patients with Fisher Groups
×
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
现在去查看 取消
×
提示
确定
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
已复制链接
已复制链接
快去分享给好友吧!
我知道了
×
扫码分享
扫码分享
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 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 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1