Synthesis and Bioassay of New Urea and Thiourea Derivatives of 4-Aminobenzohydrazide

IF 0.8 4区 化学 Q4 CHEMISTRY, ORGANIC Russian Journal of Organic Chemistry Pub Date : 2024-10-14 DOI:10.1134/S1070428024070108
K. Pushpa Kumar, M. Varalakshmi, Y. B. Kiran, U. Nagarjuna, M. Rajaswi Devi, D. Venkataramana Reddy, C. Naga Raju
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Abstract

A series of new urea 3a–3d and thiourea derivatives 5a–5f have been synthesized in high yields (77–88%) by the reaction of substituted aryl isocyanates 2a–2d and substituted aryl isothiocynates 4a–4f with 4-aminobenzoic hydrazide 1. The structures of all the synthesized compounds were characterized by IR, NMR (1H and 13C), mass and elemental analyses. The synthesized compounds were screened for their anti-microbial activity. The present study revealed that Gram-negative and positive bacteria such as Escherichia coli and Streptococcus aureus were more susceptible to the solvent extracts. The methanol and acetone extracts of the newly synthesized compounds were evaluated for in vitro antibacterial activity against human pathogenic bacteria Escherichia coli and Streptococcus aureus and antifungal activity against Aspergillus niger and Aspergillus oryzae. Compound 5e have exhibited good antibacterial and antifungal activity.

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4-Aminobenzohydrazide 的新型尿素和硫脲衍生物的合成与生物测定
通过取代的芳基异氰酸酯 2a-2d 和取代的芳基异硫代氰酸酯 4a-4f 与 4-氨基苯甲酸酰肼 1 反应,合成了一系列新的脲 3a-3d 和硫脲衍生物 5a-5f,收率高达 77-88%。通过红外光谱、核磁共振(1H 和 13C)、质量和元素分析对所有合成化合物的结构进行了表征。对合成的化合物进行了抗微生物活性筛选。本研究发现,大肠杆菌和金黄色葡萄球菌等革兰氏阴性和阳性细菌对溶剂提取物更易感。对新合成化合物的甲醇和丙酮萃取物进行了体外抗菌活性评估,以检测其对人类致病菌大肠杆菌和金黄色链球菌的抗菌活性,以及对黑曲霉和米曲霉的抗真菌活性。化合物 5e 具有良好的抗菌和抗真菌活性。
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来源期刊
CiteScore
1.40
自引率
25.00%
发文量
139
审稿时长
3-6 weeks
期刊介绍: Russian Journal of Organic Chemistry is an international peer reviewed journal that covers all aspects of modern organic chemistry including organic synthesis, theoretical organic chemistry, structure and mechanism, and the application of organometallic compounds in organic synthesis.
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