以二苯并-18-冠醚-6 为原料合成新的嘧啶硫化合物并评估其抗菌活性

Zena Abdali, Raheem Jameel Mahesein
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引用次数: 0

摘要

在本研究中,我们提出了一种从前体化合物二苯并-18-冠醚-6(DB-18-CE-6)生产噻吩嘧啶化合物(包括 P-OH-噻吩嘧啶、P-NO2-噻吩嘧啶和 P-Cl2-噻吩嘧啶)的新型合成方法。这些噻吩嘧啶化合物在各种应用领域,特别是作为抗菌剂方面具有巨大的潜力。合成过程涉及 DB-18-CE-6 衍生的 alpha-beta 不饱和酮与硫脲在碱性介质中发生反应,从而成功实现环化。评估了合成的噻吩嘧啶化合物对链球菌、葡萄球菌和变形杆菌等常见细菌菌株的抗菌活性,并与抗生素阿奇霉素进行了比较。结果表明,噻吩并嘧啶化合物(Z、Z1、Z2、Z3)表现出卓越的抗菌活性,超过了阿奇霉素,凸显了它们作为抗击细菌感染的有效替代品的潜力。这项研究为开发抗菌剂开辟了新途径,并强调了噻吩嘧啶化合物在解决细菌耐药性问题方面的重要意义。 亮点:从 DB-18-CE-6 中新合成噻吩嘧啶化合物。 评估对链球菌、葡萄球菌和变形杆菌的抗菌活性。 嘧啶硫化物作为有效抗菌剂的潜力。 关键词:嘧啶硫化物;抗菌活性;DB-18-CE-6;新型合成;细菌耐药性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Novel Synthesis of Thiopyrimidine Compounds from Dibenzo-18-Crown-6 and Evaluation of Antibacterial Activity
In this study, we present a novel synthesis approach for the production of thiopyrimidine compounds, including P-OH-Thiopyrimidine, P-NO2-Thiopyrimidine, and P-Cl2-Thiopyrimidine, from the precursor compound dibenzo-18-crown-6 (DB-18-CE-6). These thiopyrimidine compounds have shown significant potential for various applications, particularly as antibacterial agents. The synthesis involved the reaction of DB-18-CE-6-derived alpha-beta unsaturated ketones with thiourea in a basic medium, resulting in successful cyclization. The synthesized thiopyrimidine compounds were evaluated for their antibacterial activity against common bacterial strains, including Streptococcus, Staphylococcus, and Proteus, and compared to the antibiotic Azithromycin. The results demonstrated that the thiopyrimidine compounds (Z, Z1, Z2, Z3) exhibited excellent antibacterial activity, surpassing Azithromycin, and highlighting their potential as effective alternatives to combat bacterial infections. This research opens new avenues for the development of antibacterial agents and emphasizes the significance of thiopyrimidine compounds in addressing bacterial resistance issues. Highlights :  Novel synthesis of thiopyrimidine compounds from DB-18-CE-6. Evaluation of antibacterial activity against Streptococcus, Staphylococcus, and Proteus. Potential of thiopyrimidine compounds as effective antibacterial agents. Keywords : Thiopyrimidine compounds, Antibacterial activity, DB-18-CE-6, Novel synthesis, Bacterial resistance.
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