Acute toxicity and anti-inflammatory activity of bis-thiourea derivatives

IF 2.1 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY Open Chemistry Pub Date : 2024-05-14 DOI:10.1515/chem-2024-0033
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
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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(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.
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双硫脲衍生物的急性毒性和抗炎活性
在当前的研究工作中,通过异硫氰酸盐和二胺在干丙酮中的缩合反应合成了双硫脲衍生物,形成了 SK1(1,2-双(N-苯甲酰基硫脲基)苯)、SK2(1,3-双(N-苯甲酰基硫脲基)苯)和 SK3(1,4-双(N-苯甲酰基硫脲基)苯)。新合成衍生物的结构通过熔点和 1HNMR 等光谱技术得到了确认。对合成的化合物进行了急性毒性测试,证明其无毒性。通过体外脂氧合酶抑制研究、分子对接、体内卡拉胶诱导的爪水肿试验和组胺诱导的水肿试验,进一步测试了这些衍生物的抗炎性能。总体观察结果表明,化合物 SK1 和 SK3 具有良好的抗炎潜力,而化合物 SK2 则是一种良好的抗炎剂。
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来源期刊
Open Chemistry
Open Chemistry CHEMISTRY, MULTIDISCIPLINARY-
CiteScore
3.80
自引率
4.30%
发文量
90
审稿时长
6 weeks
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.
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