Muhammad Naveed Umar, Muhammad Shoaib, Mehreen Ghias, Shakila Bibi, Muhammad Zahoor, Sher Wali Khan, Riaz Ullah, Essam A. Ali, Naila Gulfam, Syed Wadood Ali Shah
{"title":"双硫脲衍生物的急性毒性和抗炎活性","authors":"Muhammad Naveed Umar, Muhammad Shoaib, Mehreen Ghias, Shakila Bibi, Muhammad Zahoor, Sher Wali Khan, Riaz Ullah, Essam A. Ali, Naila Gulfam, Syed Wadood Ali Shah","doi":"10.1515/chem-2024-0033","DOIUrl":null,"url":null,"abstract":"In the current work, bis-thiourea derivatives have been synthesized through condensation reaction between isothiocynates and diamines in dry acetone to form SK1 (1,2-bis(<jats:italic>N</jats:italic>-benzoylthioureido) benzene), SK2 (1,3-bis(<jats:italic>N</jats:italic>-benzoylthioureido) benzene), and SK3 (1,4-bis(<jats:italic>N</jats:italic>-benzoylthioureido) benzene). The structures of new synthesized derivatives were confirmed through melting point and spectroscopic technique such as <jats:sup>1</jats:sup>HNMR only. The synthesized compounds were assessed for acute toxicity test and are proved free of toxicity. The derivatives were further tested as anti-inflammatory agents by <jats:italic>in vitro</jats:italic> lipoxygenase enzyme inhibition studies, molecular docking, and <jats:italic>in vivo</jats:italic> carrageenan-induced paw edema assay, and histamine-induced edema test. The overall observations presented that compounds SK1 and SK3 possess promising anti-inflammatory potential, while compound SK2 is found to be a good anti-inflammatory agent.","PeriodicalId":19520,"journal":{"name":"Open Chemistry","volume":"52 1","pages":""},"PeriodicalIF":2.1000,"publicationDate":"2024-05-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Acute toxicity and anti-inflammatory activity of bis-thiourea derivatives\",\"authors\":\"Muhammad Naveed Umar, Muhammad Shoaib, Mehreen Ghias, Shakila Bibi, Muhammad Zahoor, Sher Wali Khan, Riaz Ullah, Essam A. Ali, Naila Gulfam, Syed Wadood Ali Shah\",\"doi\":\"10.1515/chem-2024-0033\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"In the current work, bis-thiourea derivatives have been synthesized through condensation reaction between isothiocynates and diamines in dry acetone to form SK1 (1,2-bis(<jats:italic>N</jats:italic>-benzoylthioureido) benzene), SK2 (1,3-bis(<jats:italic>N</jats:italic>-benzoylthioureido) benzene), and SK3 (1,4-bis(<jats:italic>N</jats:italic>-benzoylthioureido) benzene). The structures of new synthesized derivatives were confirmed through melting point and spectroscopic technique such as <jats:sup>1</jats:sup>HNMR only. The synthesized compounds were assessed for acute toxicity test and are proved free of toxicity. The derivatives were further tested as anti-inflammatory agents by <jats:italic>in vitro</jats:italic> lipoxygenase enzyme inhibition studies, molecular docking, and <jats:italic>in vivo</jats:italic> carrageenan-induced paw edema assay, and histamine-induced edema test. The overall observations presented that compounds SK1 and SK3 possess promising anti-inflammatory potential, while compound SK2 is found to be a good anti-inflammatory agent.\",\"PeriodicalId\":19520,\"journal\":{\"name\":\"Open Chemistry\",\"volume\":\"52 1\",\"pages\":\"\"},\"PeriodicalIF\":2.1000,\"publicationDate\":\"2024-05-14\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Open Chemistry\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://doi.org/10.1515/chem-2024-0033\",\"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":"Open Chemistry","FirstCategoryId":"92","ListUrlMain":"https://doi.org/10.1515/chem-2024-0033","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
Acute toxicity and anti-inflammatory activity of bis-thiourea derivatives
In the current work, bis-thiourea derivatives have been synthesized through condensation reaction between isothiocynates and diamines in dry acetone to form SK1 (1,2-bis(N-benzoylthioureido) benzene), SK2 (1,3-bis(N-benzoylthioureido) benzene), and SK3 (1,4-bis(N-benzoylthioureido) benzene). The structures of new synthesized derivatives were confirmed through melting point and spectroscopic technique such as 1HNMR only. The synthesized compounds were assessed for acute toxicity test and are proved free of toxicity. The derivatives were further tested as anti-inflammatory agents by in vitro lipoxygenase enzyme inhibition studies, molecular docking, and in vivo carrageenan-induced paw edema assay, and histamine-induced edema test. The overall observations presented that compounds SK1 and SK3 possess promising anti-inflammatory potential, while compound SK2 is found to be a good anti-inflammatory agent.
期刊介绍:
Open Chemistry is a peer-reviewed, open access journal that publishes original research, reviews and short communications in the fields of chemistry in an ongoing way. The central goal is to provide a hub for researchers working across all subjects to present their discoveries, and to be a forum for the discussion of the important issues in the field. The journal is the premier source for cutting edge research in fundamental chemistry and it provides high quality peer review services for its authors across the world. Moreover, it allows for libraries everywhere to avoid subscribing to multiple local publications, and to receive instead all the necessary chemistry research from a single source available to the entire scientific community.